Nan-Horng (Stan) Lin, Ph.D.
432 W. Sycamore Dr.
Vernon Hills, IL 60061
Residence: (847) 918-0742
Cell: (847) 668-0072
E-mail: linn542002@yahoo.com
SUMMARY
A creative, target oriented manager who delivered results. Experience in identifying clinical candidates as well
as building and leading highly productive research team in drug discovery and CRO organizations (see
accomplishment summary). Background includes synthetic organic chemistry, medicinal chemistry, new target
identification, hit to lead optimization and general research management in pharmaceutical and CRO companies.
A skilled researcher and manager who can resolve complicated medicinal chemistry problems and deliver
clinical candidates in drug discovery research area.
Keyword: drug discovery, medicinal chemist, group leader, pharmaceutical, biotechnology, SAR, hit to lead,
synthesis, organic chemistry, structure-activity, lead optimization, project leader, manager, inhibitors,
neuroscience, pre-clinical, process chemistry, receptors, oncology, HTS, high throughput screening, predevelopment.
PROFESSIONAL EXPERIENCE
Crown Bioscience Inc
A Contract Research and Biopharmaceutical Organization
Senior Vice President




Lead the Small Molecule Drug Discovery Division (SMDD) that includes Chemistry, Structure biology,
Computational chemistry, DMPK and Pre-formulation departments. Responsible for the integrated drug
discovery projects that collaborated with both Chinese and US pharmaceutical companies.
Responsible for targeted the annual fee for service (FFS) revenue generated in DMPK, Structure
Biology and Pre-formulation departments.
Participated in business development activities in the US and Asia regions. Work with BDs closely in
various business development activities.
Responsible for the direction of future drug discovery projects. A key member of project review
committee (chairman of committee for 2011).
Medicilon, Inc.
A Contract Research Organization
Chief Scientific Officer


2009 Nov-2011 April
Lead the whole operation of scientific organization including chemistry, biology and preclinical
divisions which consist of more than 250 scientists.
Participated in business development in the US and Asia regions
Medicilon, Inc.
A Contract Research Organization
VP, Chemistry

2011 Jun-Present
2008 Jan- 2009 Oct
Led the whole chemistry division of 188 chemists (80% of them hold Ph.D. or Ms degree).




Directed and personally involved in medicinal chemistry CRO efforts for big pharmaceutical and
midsize biotechnology companies, focusing on targets in the areas of neuroscience, metabolic diseases
and cancer.
Played an instrumental role in attracting and recruiting experienced oversea chemist as the key
member of the senior management team.
Participated in business development in the US and played a major role in securing a few FTEs within a
few months after joining the company.
Plan and execute the strategy for the whole chemistry department which consists of medicinal
chemistry, library synthesis, customer synthesis, process research and scale-up departments.
Abbott Laboratories, Abbott Park, Illinois
A Fortune 100 healthcare company
Senior Group Leader & Fellow
Cancer Research




Led 9-13 junior and senior chemists conducting chemistry research.
Made go or no-go decision in Hedgehog project in less than 6 months by synthesizing competitor’s
compounds and critically examining biological data.
Identified three novel and new chemical series in the Chk1 project by dividing chemistry group into
three sub-groups. Selected a pre-clinical candidate that has better biological profile than Pfizer’s Chk1
inhibitor from these three series. Identified two other back-up candidates for potential clinical studies in
the future.
Identify a potent and novel farnesyl transferase inhibitor, ABT-100, as clinical candidate within 1.5
years after switching to cancer research area from neuroscience by inventing a novel chemical skeleton
that possesses high FT enzymatic selectivity.
Associate Research Fellow
Neuroscience Research, Abbott Laboratories






1995-1999
Principal inventor for ABT-089, ABT-594 and ABT-259 by identifying heterocyclic pyridyl
ethers series, which is the basic chemical skeleton of these clinical candidates.
Primary inventor of ABT-089 that was approved for development as cognition enhancer (6/95) as
well as treatment for ADHD patients in 2002 by designed and synthesizing ABT-089.
Developed the process chemistry for preparation of ABT-089 in pilot plant within three month
time to speed up the clinical trial.
Responsible for identification of ABT-594 (approved for development as treatment for acute and
chronic pain, 12/96) and ABT-259, a second generation of nicotinic acetylcholine receptor
modulators by conducting thorough SAR studies and discovering the key piece in both ABT-549
and ABT-259.
Research Investigator
Neuroscience Research, Abbott laboratories

1999 -2007 Dec.
1990 to 1995
Authored numerous patent applications and received several patents related to novel nicotinic
acetylcholine receptor modulators.
Made significant contributions to the identification of ABT-418 in a short period of time (approved for
development as cognition enhancer, 8/93).
Responsible for development of process chemistry procedures for preparation of ABT-418 in large
quantities. Reduced the production cost dramatically and made it economically cheaper than nicotine.
Received several patents for this chemistry process.
Bayer USA (formally Miles Laboratories), Inc. Elkhart, Indiana.
A Fortune 100 company
2
1986 to 1990
Senior Research Scientist
Diagnostic Division
 Identified three tetrazonium salts that possess the desired wavelengths and extinction coefficients for
diagnostic division at Bayer USA in timely fashion by designing and synthesizing special dyes that
have broad wavelength. Due to their superior properties, they were produced commercially in large
quantities and applied to the preparation of glucometer testing strips.
Education
Postdoctoral, University of California, Irvine
Total synthesis of pumiliotoxin A under Professor Larry Overman’s supervision
Ph.D., Indiana University, Bloomington
Under the supervision of Professor Paul Grieco: Synthesis of natural products such as prostaglandin,
sixteen membered-ring macrolide-tylonolide.
M. S., National Taiwan University
Under the supervision of Prof. Yao-Tung Lin: Isolation and identification of several new terpenes from
barks of hardwoods.
B. S., National Chung-Hsing University
ACCOMPLISHMENT SUMMARY
Identified the following four clinical candidates. The detailed description of the discovery process is indicated
below:
ABT-418
ABT-418 is a cholihergic channel activator that was identified in 1991 and approved for development as
cognition enhancer, in August 1993. This compound has reduced side-effect liabilities compared to the (-)nicotine. In addition, it elicits a variety of behavior effects including cognitive-enhancing and anxiolytic-like
activity, in preclinical model. Made significant contributions to the identification of ABT-418 as evident in the
papers that were published during the period of 1994-1995. Responsible for development of process chemistry
procedures for large scale preparation of ABT-418, accelerating the clinical development tremendously due to
the easy synthesis and low cost arising from this process. The chemistry provides the final product cost which
is lower than nicotine itself.
ABT-089
ABT-089 is an orally bioavailable back-up candidate for ABT-418. It possesses the core NCCX framework
in the structure. Based on the structure of MCC, developed this series of compound in 1991. The first lead
(17 nM) was identified in January 1992. A further improvement (0.2 nM) was achieved by my associate a
few months later. The first paper in this series was published in 1996 (see attachment). After identification of
this series, kept the pyrrolidine moeity constant and started the modification on the pyridine ring because the
parent compound did show cardiovascular liabilities. The SAR studies were published in 1999. Identified
ABT-089 as an orally bioavailable cholinergic channel modulator. This compound was approved for the
development as cognition enhancer in June 1995. It was also approved as clinical candidate for ADHD in
July, 1999. This work was published in 1997.
ABT-594
3
Also responsible for identification of ABT-594 which was approved for development as treatment for acute
and chronic pain in 1996. My group had identified 6-chloro pyridine as the most potent pyridyl moiety in this
series based on the SAR studies described above. Coupled the SAR data in the parent series (see publication
in 1996) and this information, we conducted the synthesis of ABT-594. This work was published in 1998.
ABT-594 was also covered in the patent filed by me in 1995 and issued in 1999.
ABT-100
ABT-100 is a potent and novel farnesyl tramsferase inhibitor. Collaborated with associate and initially
developed novel carbon triaryl series, which possesses potent biological activities. To broadly cover the
patent position, new ortho pyridone phenyl series of FTI were designed and implemented. In addition,
several novel o-alkyl substituted, pyridine and pyridone analogs were synthesized to improve the PK profiles.
We initiated and synthesized the biphenyl series with either acetylene or ether linkage that lead to the
identification of clinical candidates ABT-100.
AWARDS
Outstanding Researcher Team Award, Abbott Laboratories
President Award, Abbott Laboratories
Chairman Award, Abbott Laboratories
Miles Diagnostic Science and Technology Award, Miles Laboratories, Inc.
Miles Diagnostic Science and Technology Award, Miles Laboratories, Inc.
PROFESSIONAL ACTIVITIES
Scientific reviewer for Journal of Medicinal Chemistry
Scientific reviewer for Boorganic & Medicinal Chemistry
Scientific reviewer for Synthesis
Scientific reviewer for European Journal of Medicinal Chemistry
Scientific reviewer for Journal of Organic Chemistry
PROFESSIONAL AFFILIATIONS
American Chemical Society
Chinese Chemical Society
American Association for the Advancement of Science
MANAGEMENT COURSES
Miles Practices I
Miles Laboratories, Inc.
Leadership Effective Training
Miles Laboratories, Inc.
Technical Leadership
4
2006
2001
1996
1989
1987
Abbott Laboratories, Inc.
ADDENDUM
PATENTS
1.
Preparation of 2,5-dithienlpyrrole monomers for semi-conducting oligomers. James Albarella, NanHorng Lin. Eur. Pat. Appl. EP 389904, 1990.
2.
Dithiophenylpyrrole derivative monomers for preparing semiconducting polymers. Nan-Horng Lin,
James Albarella. U. S. patent number, 5,021,586, 1991.
3.
Semi-conducting oligomers and method relating thereto. Nan-Horng Lin, James Albarella. U. S. patent
number 5,068,535, 1991.
4.
Analytical methods using tetrazolium salt indicators having a reflectance plateau. Nan-Horng Lin,
Robert Hatch, Scott Ruetten, Klaus Wehling. U. S. patent number 5,126,275,1992.
5.
Isoxazole and isothiazole compounds that enhance cognitive function. Dave Garvey, George Carrera,
Steve Arneric, Nan-Horng Lin; Yue-Kong Shue; Yun He. WO 9221339, December, 1992; Ireland,
921690, 1992; Portugal, 100525, 1992; EPC, 9291297, 1992; Canada, 2109585, 1992; Japan,
500624/93, 1992.
6.
Method of preparing enatiomerically pure 3-methyl-5-(1-methyl-2-(s)-pyrrolidinyl) isoxazole. NanHorng Lin, Yun He, Richard Elliott. U. S. Application number 117819, September, 1993. (Foreign
equivalent: Mexico, 937362, 1993; PCT/US 94/09734, 1994)
7.
2-Benzothiazolyl teterazolium salt indicators. Robert P. Hatch, Nan-Horng Lin, Scott Reutten. US
patent number 5,300,637, 1993.
8.
3-Pyridyloxymethyl heterocyclic ether compounds useful in controlling neurotransmitter release.
Melwyn Abreo, Nan-Horng Lin, Dave Gunn, Richard L. Elliott, David S. Garvey, Suzanne S. Lebold,
James T. Wasicak. U. S. application number 129223, 1993. (Foreign equivalent: Israel, 107184, 1993;
Mexico, 936274, 1993; Philippines, 47021, 1993).
9.
Preparation of azacycloalkyl heteroaryl ether as cholinergic channel agonist. Melwyn Abreo, NanHorng Lin, Dave Gunn, Richard L. Elliott, Suzanne A. Lebold, James T. Wasicak. WO 9408992, April,
1994; (foreign equivalent: EPC, 93923826, 1993; Canada, 2136075, 1993; Japan, 510167/94, 1993;
Korea, 94-704340, 1993).
10.
Nicotine derivatives that enhance cognitive function. Nan-Horng Lin. U. S. patent number, 5,278,176,
January, 1994.
11.
Method of preparing enatiomerically pure 3-methyl-5-(1-alkyl-2-(S)-pyrrolidinyl) isoxazoles. NanHorng Lin, Yun He, R. Elliott, M. S. Chorghade, S. J. Wittenberger, W. H. Bunnelle, B. A. Narayanan,
P. R.. Singam, T. K. J. Esch, D. O. Beer, C. C. Witzig, T.C. Herzig, A. V.Rao. WO 9507277, Mar. 1995.
12.
Isoxazole, isothiazole and pyrazole compounds that enhance cognitive function. David S. Garvey,
George Carrera, Steve Arneric, Nan-Horng Lin, Yue-Kong Shue, Yun He, Edmund L. Lee, Suzanne A.
Lebold. U. S. patent number 5,409,946, April, 1995.
13.
Method of preparing enatiomerically pure 3-methyl-5-(1-alkyl-2-(S)-pyrrolidinyl)isoxazoles. NanHorng Lin, Yun He, Richard Elliott, M. S. Chorghade, S. J. Wittenberger, W. H. Bunnelle, B. A.
5
Narayanan, P.R. Singam, T. K. J. Esch, D.O. Beer, D.O. Herzig, T.C. Rao, A. V. U. S. patent number,
5,424,444, June, 1995.
14.
2-((Nitrophenoxymethyl)pyrrolidine compounds that enhance cognitive function. Nan-Horng Lin,
Richard Elliott, David Gunn, Mark Holladay, Hana Kopecka. U. S. patent number 5,472,958, December,
1995.
15.
Intermediates for the preparation of enatiomerically pure 3-methyl-5-(1-(C1-C3)alkyl-2-pyrrolidinyl)
isoxazoles. Nan-Horng Lin, Yun He, W. H. Bunnelle. U. S. patent number 5,508,418, April, 1996.
16.
Method of preparing enatiomerically pure 3-methyl-5-(1-alkyl-2-(S)-pyrrolidinyl) isoxazoles for
pharmaceutical use. Nan-Horng Lin, Yun He, S. Wittenberger. U. S. patent number, 5,516,912, May,
1996.
17.
Process for the preparation of enatiomerically pure 3-methyl-5-(1-alkyl-2-(S)-pyrrolidinyl) isoxazoles.
Nan-Horng Lin, Yun He, S. Wittenberger. U. S. patent number, 5, 424,444, June, 1996.
18.
Method of preparing enatiomerically pure 3-Methyl-5-(1-alkyl-2-(S)-pyrrolidinyl) isoxazoles. NanHorng Lin, Yun He, S. Wittenberger. U. S. patent number 5,559,242, September, 1996.
19.
Preparation of 2-[3-(pyridyloxyalkyl]azetidine and pyrrolidine as nicotinic receptor ligands.
Holladay, Mark W.; Lin, Nan-Horng; Ryther, Keith B.; He, Yun. PCT Int. Appl. WO 9640682,
December, 1996.
20.
3-Pyridyl Enantiomers And Their Use As Analgesics. Mark Holladay, Nan-Horng Lin, M. J. Dart, Hao
Bai, Y. S. Or, James Sullivan, Keith Ryther, Stephen P. Arneric, John Lynch, James T. Wasicak, WO
9825920, December, 1996.
21
3-Pyridyloxyalkyl heterocyclic ether compounds useful in controlling chemical synaptic transmission.
Nan-Horng Lin, Yun He, Yihong Li, Mark W. Holladay. U. S. patent number 5,629,325, May, 1997.
22.
Preparation of 7 -Heterocycle-Substituted Hexahydro-1H-pyrrolizine Compounds Useful In Controlling
Chemical Synaptic Transmission. James T. Wasicak, David Garvey, Nan-Horng Lin, Mark Holladay,
K. B. Ryther. US 5,733,912, March 1998.
23.
3-Pyridyl enantiomers [3-(2-azetidinylmethoxy)pyridines] and their use as analgesics. Holladay, Mark
W; Arneric, Stephen P; Bai, Hao; Dart, Michael J; Lin, Nan-Horng; Lynch, John K; Or, Yat Sun;
Ryther, Keith B.; Sullivan, James P. Wasicak, James T; Ehrlich, Paul P. PCT Int. Appl. WO 9825960,
June, 1998.
24
Furopyridine, Thienopyridine, Pyrrolopyridine and Related Pyrimidine, Pyridazine and Triazine
Compounds Useful in Controlling Chemical Synaptic Transmission. Richard L. Elliott, Keith Ryther,
Mark H. Holladay, James T. Wasicak, Jerome F. Daanen, Nan-Horng Lin, Michael J. Dart, Yun He,
Yihong Li. PCT Int. Appl WO 9846609, October, 1998.
25
Preparation of heterocyclic ether compounds as neuronal nicotinic receptor ligands. Holladay, Mark W;
Abreo, Melwyn A; Gunn, David E; Lin, Nan-Horng; Garvey, David S.; Ryther; Keith B.; Lebold,
Suzanne A.; Elliott, Richard L.; He, Yun; Wasicak, James P.; Bai, Hao, Dart, Michael J; Ehrlich, Paul
P.; Li, Yihong; Lynch, John K;. PCT Int. Appl WO 9932480, July, 1999.
26
Preparation of heterocyclic ether compounds as neuronal nicotinic receptor ligands. Nan-Horng Lin,
Mark W. Holladay, Melwyn A. Abreo, David E. Gunn, Suzanne A. Lebold, Richard L. Elliott, Yun He.
U. S. patent number 5,914,328; June, 1999.
6
27.
3-Pyridyloxymethyl Heterocyclic Ether Compounds Useful in Controlling Neurotransmitter Release.
Abreo, Melwyn A; Gunn, David E.; Lin, Nan-Horng; Garvey, David S.; Holladay, Mark W.; Ryther,
Keith B. US patent number 5,948,793, June, 1999.
28.
Furopyridine, thienopyridine pyrrolopyridine useful in controlling chemical synaptic transmission.
Elliott; Richard L.; Ryther, Keith B; Holladay, Mark W.; Wasicak, James T.; Daanen, Jerome F.; Lin,
Nan-Horng ; Dart, Michael J. ; He, Yun ; Li, Yihong . US patent 6,001,849, December, 1999.
29.
3-Pyridyl enantiomers and their use as analgesics. Holladay; Mark W; Arneric; Stephen P; Bai; Hao;
Dart; Michael J; Lin; Nan-Horng; Lynch; John K; Or; Yat Sun; Ryther; Keith B.; Sullivan; James P.
Wasicak; James T; Ehrlich; Paul P. U. S. patent number 6,133,253, October, 2000.
30.
3-Pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission.
Lin, Nan-Horng; He, Yun; Holladay, Mark W; Ryther, Keith B; Li, Yihong,; Bai, Hao. U. S. patent
number 6,127,386, October, 2000.
31.
3-Pyrrolidinyloxy-3-pyridyl ether compounds useful in controlling chemical synaptic transmission. Lin,
Nan-Horng; Li, Yihong,; Drizn, Irene ;Kincaid, John, F. ;Basha, Anwer ;Dong, Liming ;Hkeem,
Ahmed. PCT Int. Appl WO 2001019817, March, 2001.
32.
Substituted pyridine compounds useful for controlling chemical synaptic transmission. Lin, NanHorng; Dong, Liming. PCT Int. Appl WO 2001056991 A1, August, 2001.
33.
Preparation of Substituted 4-(Heteroarylmethyl)benzonitriles as Farnesyltransferase Inhibitors. Wang,
Wei-Bo; Curtin, Michael L.; Fakhoury, Stephen A.; Gwaltney, Stephen L., II; Hasvold, Lisa A.;
Hutchins, Charles W.; Li, Qui; Lin, Nan-Horng; Jennings Nelson, Lissa Taka; O'Connor, Stephen J.;
Sham, Hing L.; Sullivan, Gerald M.; Wang, Gary T.; Wang, Xilu. PCT Int. Appl. WO 200181316 A2,
November, 2001.
34.
Preparation of (Imidazolylalkyl)biphenylcarbonitriles and Analogs as Farnesyltransferase Inhibitors.
Wang, Wei-Bo; Curtin, Michael L.; Fakhoury, Stephen A.; Gwaltney, Stephen L.; Hasvold, Lisa A.;
Hutchins, Charles W.; Li, Qun; Lin, Nan-Horng; Nelson, Lissa Taka Jennings; O'Connor, Steve; Sham,
Hing L.; Sullivan, Gerard M.; Wang, Gary T.; Wang, Xilu. U.S. Pat. Appl. Publ. US 2002019527 A1,
Febraury, 2002.
35.
Synthesis of (homochiral) aminoalkoxypyridine derivatives useful for controlling chemical synaptic
transmission. Lin, Nan-Horng; Dong, Liming. U.S. Pat. Appl. Publ. US 2002058646 A1, May, 2002.
36.
Preparation of 3-Pyrrolidinyl 3-pyridyl Ethers for Selective Control of Neurotransmitter Release. Lin,
Nan-Horng; Li, Yihong; Drizin, Irene; Kincaid, John F.; Basha, Anwer; Dong, Liming; Hakeem,
Ahmed A. U.S. Pat. Appl. Publ. US 2002151712 A1, October, 2002.
37.
3-Pyridyl enantiomers and their use as analgesics. Holladay, Mark W; Arneric, Stephen P; Bai, Hao;
Dart; Michael J; Lin, Nan-Horng; Lynch, John K; Or, Yat Sun Ryther, Keith B.; Sullivan, James
P,.Wasicak, James T; Ehrlich, Paul P. U. S. patent number 6,403,575, June, 2002.
38.
3-Pyridyloxyalkyl Heterocyclic Ether Compounds with Nicotinic Cholinergic Activity, Useful in
Controlling Chemical Synaptic Transmission. Nan-Horng Lin, Yun He, Yihong Li, Keith Ryther, Mark
W. Holladay, Hao Bai. U. S. patent number 6,437,138, August, 2002.
39.
Imidazole and Thiazole Derivatives of Benzonitrile as Farnesyltransferase Inhibitors, and Their
Preparation and Use for The Treatment of Cancer. Claiborne, Akiyo K.; Gwaltney, Stephen L.; Hasvold,
Lisa A.; Li, Qun; Li, Tongmei; Lin, Nan-Horng; Mantei, Robert A.; Rockway, Todd W.; Sham, Hing
L.; Sullivan, Gerard M.; Tong, Yunsong; Wang, Gary; Wang, Le; Wang, Xilu; Wang, Wei-Bo. U.S. Pat.
Appl. Publ US 2002115640 A1, August, 2002.
7
40.
Imidazole and Thiazole Derivatives of Benzonitrile as Farnesyltransferase Inhibitors, and Their
Preparation and Use for The Treatment of Cancer. Claiborne, Akiyo K.; Gwaltney, Stephen L.; Hasvold,
Lisa A.; Li, Qun; Li, Tongmei; Lin, Nan-Horng; Mantei, Robert A.; Rockway, Todd W.; Sham, Hing
L.; Sullivan, Gerard M.; Tong, Yunsong; Wang, Gary; Wang, Le; Wang, Xilu; Wang, Wei-Bo. U.S. Pat.
Appl. Publ US 2003087940 A1. May, 2003.
41.
Preparation of 3-Heteroarylmethylene-1,3-dihydro-2H-indol-2-ones as Protein Kinase Inhibitors. Lin,
Nan-Horng; Sham, Hing L.; Xia, Ping. PCT Int. Appl. 2003, WO 200 0351838 A2.
42.
Preparation of 3-heteroarylmethylene-1,3-dihydro-2H-indol-2-ones as protein kinase inhibitors. Lin,
Nan-Horng, Sham, Hing L.; Xia, Ping. US 2003119839 A1, June, 2003.
43.
Preparation of 3-heteroarylmethylene-1,3-dihydro-2H-indol-2-ones as protein kinase inhibitors. Lin,
Nan-Horng; Sham, Hing L.; Xia, Ping. US 2003162785 A1, August, 2003.
44.
Substituted pyridine compounds useful for controlling chemical synaptic transmission. Lin, NanHorng; Dong, Liming. US patent number 6,656,958, December, 2003.
45.
Preparation of urea kinase inhibitors. Li, Goaquan; Li, Qun; Li, Tongmei; Lin, Nan-Horng; Mantei,
Robert A.; Sham, Hing L.; Wang, Gary T. U.S. Pat. Appl. Publ, US 20040219 A1, February, 2004.
46.
Preparation of dibenzo[b,e][1,4]diazepin-11-ones as kinase inhibitors for treatment of cancer. Hasvold,
Lisa A.; Hexamer, Laura; Li, Gaoquan; Lin, Nan-Horng; Sham, Hing; Sullivan, Gerard M.; Wang, Le;
Xia, Ping. PCT Int. Appl. WO 2004076424 A1, September, 2004.
47.
Preparation of indeno[1,2-c]pyrazoles and related fused pyrazole kinase inhibitors as anticancer agents.
Tong, Yunsung; Claiborne, Akiyo K.; Li, Gaoquan; Lin, Nan-Horng; Sham, Hing; Tao, Zhi-Fu; Sowin,
Tom. PCT Int. Appl. WO 2004080973 A1, September, 2004.
48.
Heterocyclic kinase inhibitors. Hasvold, Lisa A.; Hexamer, Laura; Li, Gaoquan; Lin, Nan-Horng;
Sham, Hing; Sowin, Tom; Sullivan, Gerard M.; Wang, Le; Xia, Ping. PCT Int. Appl. WO 2004076424
A1, 2004.
49.
Preparation of urea kinase inhibitors. Li, Goaquan; Li, Qun; Li, Tongmei; Lin, Nan-Horng; Mantei,
Robert A.; Sham, Hing L.; Wang, Gary T. U.S. Pat. Appl. Publ, US 2004259885 A1, December, 2004.
50.
Preparation of dibenzo[b,e][1,4]diazepin-11-ones as kinase inhibitors for treatment of cancer. Hasvold,
Lisa A.; Hexamer, Laura; Li, Gaoquan; Lin, Nan-Horng; Sham, Hing; Sullivan, Gerard M.; Wang, Le;
Xia, Ping. U.S. Pat. Appl. Publ. US 2004254159 A1, December, 2004.
51.
Protein Kinase Inhibitors. Nan-Horng Lin; Hing Sham, Ping Xia. US patent number, 6,797,825,
September, 2004.
52.
A preparation of macrocyclic N-(heteroaryl)urea derivatives, useful as kinase inhibitors. Tao, Zhi-Fu;
Lin, Nan-Horng; Wang, Le; Sowin, Thomas J. U.S. Pat. Appl. Publ. US 2005096324 A1, May,
2005.
53.
Preparation of substituted macrocyclic diaryl urea kinase inhibitor as potent anticancer agents. Lin, NanHorng; Li, Gaoquan; Przytulinska, Magdalenna K.; Sowin, Thomas J.; Sullivan, Gerard M.; Tao, ZhiFu; Tong, Yunsong; Wang, Le. US 20050215556 A1, September, 2005.
54.
Macrocyclic kinase inhibitors. Lin, Nan-Horng; Li, Gaoquan; Przytulinska, Magdalenna K.; Sowin,
Thomas J.; Sullivan, Gerard M.; Tao, Zhi-Fu; Tong, Yunsong; Wang, Le. US patent number, 7,163,939,
2007.
8
55.
Farnesyltransferase Inhibitors. Claiborne, Akiyo K.; Gwaltney, Stephen L.; Hasvold, Lisa A.; Li, Qun;
Li, Tongmei; Lin, Nan-Horng; Mantei, Robert A.; Rockway, Todd W.; Sham, Hing L.; Sullivan, Gerard
M.; Tong, Yunsong; Wang, Gary; Wang, Le; Wang, Xilu; Wang, Wei-Bo. US patent number,
7,211,595, May, 2007.
56.
INHIBITORS OF POLO-LIKE KINASES. Diebold, Robert B; Djuric; Stevan W.; Giranda; Vincent L.;
; Hexamer; Laura A.; Lin; Nan-Horng ; Miyashiro; Julie M. ; Penning; Thomas D. ; Przytulinska;
Magdalena ; Sowin; Thomas J.; Sullivan; Gerard M.; Tao; Zhi-Fu; Tong; Yunsong ; Vasudevan; Anil;
Wang; Le ; Woods; Keith W.; Xia; Zhiren; Zhang; Henry Q. US 20080015192 A1, Januaryr, 2008.
57.
PIM kinase Inhibitors as cancer chemotherapeutics. Pennig, Thomas D;
Hasvold, Lisa; Hexamer, Laura A; Giranda, Vincent L; Lin, Nan-horng; Tao, Zhi-fu; Wang,Le.
WO/2008/082839, 2008.
58.
Farnesyltransferase Inhibitors. Claiborne, Akiyo K.; Gwaltney, Stephen L.; Hasvold, Lisa A.; Li, Qun; Li,
Tongmei; Lin, Nan-Horng; Mantei, Robert A.; Rockway, Todd W.; Sham, Hing L.; Sullivan, Gerard M.;
Tong, Yunsong; Wang, Gary; Wang, Le; Wang, Xilu; Wang, Wei-Bo. US patent number, 7,323,570,
Jan, 2008.
59.
Fused tri and tetra-cyclic pyrazole kinase inhibitors. Tong, Yunsung; Claiborne, Akiyo K.; Li, Gaoquan;
Lin, Nan-Horng; Sham, Hing; Tao, Zhi-Fu; Sowin, Tom. US patent number, 7,320,986, January, 2008.
60. Heterocyclic kinase inhibitors. Hasvold, Lisa A.; Hexamer, Laura; Li, Gaoquan; Lin, Nan-Horng; Sham,
Hing; Sullivan, Gerard M.; Wang, Le; Xia, Ping. US patent number, 7,456,169, November, 2008.
61. Preparation of spiroheterocycles as filamin A (FLNA) binding antiinflammatory analgesics. Burns Barbier,
Lindsay; Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. PCT Int. Appl. WO 2010051476 A1, May
2010
62. Preparation of heterocycles as anti-inflammatory and analgesic agents. Burns Barbier, Lindsay; Wang,
Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. PCT Int. Appl. WO 2010051497 A1 May, 2010
63. Preparation of filamin A-binding heterocycles as analgesics. Burns Barbier, Lindsay; Wang, Hoau-Yan;
Lin, Nan-Horng; Blasko, Andrei. PCT Int. Appl. WO 2010051374 A1, May, 2010
64. Preparation of 2,3-dihydroxypropanamine derivatives as μ opioid receptor (MOR) agonists that binds
filamin A for the treatment of pain and inflammation. Burns Barbier, Lindsay; Wang, Hoau-Yan; Lin, NanHorng; Blasko, Andrei. US 20100279997, 2010
65. Preparation of methylenedioxyisoquinolines as analgesics that bind filamin a. Barbier, Lindsay Burns;
Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. US 20100280061A1, 2010
66. Preparation of heterocyclic analgesics that bind filamin A and also act as μ-opioid receptor agonists. Burns
Barbier, Lindsay; Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. US 20100280057A1, 2010
67. Preparation of spiroheterocycles as filamin A-binding μ-opioid receptor agonists for use as antiinflammatory
analgesics. Burns Barbier, Lindsay; Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. US 20110105481,
2011
68. Preparation of spiroheterocycles as filamin A (FLNA) binding antiinflammatory analgesics. Barbier,
Lindsay Burns; Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei. US 20110105547, 2011
9
PRESENTATIONS
1
Total synthesis of the sixteen membered ring macrolide tylonolide hemiacetal. Nan-Horng Lin. Indiana
University, April, 1983
2.
Enantioselective total synthesis of (+)-pumiliotoxin A. Nan-Horng Lin, Larry E. Overman. 1984,
Abstract of papers of the American Chemical Society, 184: 192-Org.
3.
Total synthesis of the sixteen membered ring macrolide tylonolide hemiacetal. Nan-Horng Lin.
National Chung-Hsing University, December, 1987
4.
a. Tetrazolium salts and their use in diagnostic test ; b. Enantioselective total synthesis of (+)pumiliotoxin A using vinylsilane cyclization methodology. Nan-Horng Lin. Fu Jern University,
December, 1987
5.
Synthesis and evaluation of nicotine analogs as neural nicotinic receptor ligands. Nan-Horng Lin, D.
Anderson; E Cadman; D. Garvey; S. Arneric. 1992, Abstract of papers of the American Chemical
Society, 204: 78-Med.
6.
A short, efficient synthesis of a novel cholinergic cognition enhances. Yun. He, Nan-Horng Lin, Hana.
Kopecka, Richard Elliott. 1994, Abstract of papers of the American Chemical Society, 207:330-Org.
7.
Isoxazole and isothiazole ligands that interact with neuronal cholinergic channel receptors. David S.
Garvey, James Wasicak, Nan-Horng Lin, Yun He, Richard Elliott, Ann-Marie Hettinger, Suzanne
Lebold, David J. Anderson, Evelyn D. Cadman, Joanna L. Raszkiewicz, James P. Sullivan, Stephen P.
Arneric and Michael Williams. 1994, Abstract of papers of the American Chemical Society, 207: 176Med.
8.
Synthesis and structure-activity relationship of pyrrolidine-modified analogs of ABT-418, a potent
cholinergic channel activator. Nan-Horng Lin, Yun He, David J. Anderson, James T. Wasicak, Richard
Kasson, David Sweeny and James P. Sullivan. 1994, Abstract of papers of the American Chemical
Society, 208: 199-Med.
9.
Synthesis and receptor binding of novel cholinergic channel ligands as potential cognition enhancers.
Nan-Horng Lin, Yun He, David. J. Anderson, Dave S. Garvey, James T. Wasicak, James P. Sullivan,
Stephen P. Arneric. 1994, Abstract of papers of the Society for Neuroscience, 24: 009604.
10.
Synthesis and structure- activity relationships of pyrrolidine-modified analogs of ABT-418, a potent
cholinergic channel activator. Nan-Horng Lin, Yun He, Yihong Li, James T. Wasicak, David J.
Anderson, Jeffrey E. Campbell, James P. Sullivan, Stephen P. Arneric. 1995, Abstract of papers of the
American Chemical Society, 210: 229-Med.
11.
3-Pyridyl ethers as novel ligands with subnanomolar affinity for neuronal nicotinic acetylcholine
receptors (nAChRs). Nan-Horng Lin, Melwyn A. Abreo, David E. Gunn, David S. Garvey, Ann Marie
Hettinger, Richard L. Elliott, Suzanne A. Lebold, Mark W. Holladay, David J. Anderson, Diana
Donnelly-Roberts, James P. Sullivan, Stephen P. Arneric and Michael Williams. 1995, Abstract of
papers of the American Chemical Society, 210: 142-Med.
12.
3-Pyridyl ethers as novel high affinity neuronal nicotinic acetylcholine receptor (nAChR) ligands. NanHorng Lin, Melwyn A. Abreo, David E. Gunn, David S. Garvey, Ann Marie Hettinger, Richard L.
Elliott, Suzanne A. Lebold, Mark W. Holladay, David J. Anderson, Diana Donnelly-Roberts, James P.
Sullivan, Stephen P. Arneric and Michael Williams. 1995, Abstract of papers of the Society for
Neuroscience, 25: 03285.
13.
Structure-activity and molecular modeling studies on nicotinic acetylcholine receptor (nAChR) ligands.
Mark W. Holladay, J. F. Daanen, H. Bai, Y. He, Suzanne A. Lebold, Patricia A. Palvik, James T.
10
Wasicak, David E. Gunn, Nan-Horng Lin, Melwyn A. Abreo, David S. Garvey,Y.C. Martin, David J.
Anderson, Jeffrey E. Campbell, Diana Donnelly-Roberts, Marietta Piattoni-Kaplan, James P. Sullivan,
Michael Williams and Stephen P. Arneric. 1995, Abstract of papers of the American Chemical Society,
210: 114-Med.
14.
2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands.
Richard L. Elliott, Hana Kopecka, David E. Gunn, Nan-Horng Lin, David S. Garvey, Keith B. Ryther,
Mark W. Holladay, David J. Anderson, Jeffrey E. Campbell, Diana Donnelly-Roberts, Marietta PiattoniKaplan, James P. Sullivan, and Stephen P. Arneric. 1995, Abstract of papers of the American Chemical
Society, 210: 143-Med.
15.
Synthetic and pharmacological studies on neurotoxic Delphinium alkaloids. John. M. Jacyno, NanHorng Lin, Mark W. Holladay, James P. Sullivan. May, 1995, Tenth Annual Penn State Symposium in
Plant Physiology.
16.
A novel series of 3-pyridylethers as ligands with subnanomolar affinity for brain nicotinic acetylcholine
receptors. Melwyn A Abreo, Nan-Horng Lin, David S. Garvey, Mark W. Holladay, James T. Wasicak,
Anne-Marie Hettinger, Diana Donnelly-Roberts, David J. Anderson, Marietta Piattoni-Kaplan, Jeffrey E.
Campbell, James P. Sullivan and Stephen P. Arneric. Strausbourg, France, 1995, Medicinal Chemistry
Approaches to Alzheimer's Disease and Other Dementias.
17.
Neuronal nicotinic acetylcholine receptor (nAChR) diversity and therapeutic potential of selective
ligands. Stephen P. Arneric, Tony Bannon, J. Brioni, Clark Briggs, Michael Decker, Richard Elliott, M
Gopalakrishnan, Mark W. Holladay, Suzanne A. Lebold, Nan-Horng Lin, D. Donnelly-Roberts, James
P. Sullivan, Michael Williams. 1995, Abstract of papers of the American Chemical Society, 210: 113Med.
18.
Structure-Activity Studies on ABT-089 : An Orally Bioavailable 3-Pyridyl Ether. Nan-Horng Lin,
David E. Gunn, Keith B. Ryther, David S. Garvey, Diana L. Donnelly-Roberts, Michael W. Decker,
Jorge D. Brioni, Michael J. Buckley, A. David Rodrigues, Kennan G. Marsh, David J. Anderson, James
P. Sullivan, Michael Williams, Stephen P. Arneric, Mark W. Holladay. 1996, Abstract of papers of the
American Chemical
19.
Cholinergic Channel Modulators as Potential Treatment for Alzheimer's Disease. Mark W. Holladay,
Nan-Horng Lin, Michael J. Dart, James T. Wasicak, Jerry D. Daanen, Keith B. Ryther, Edmund Lee,
Richard L. Elliott, David S. Garvey, Michael W. Decker, Kennan C. Marsh, A David. Rodrigues, Gary
Rotert, Diana Donnelly-Roberts, David J. Anderson, Marietta Piattoni-Kaplan, James P. Sullivan
Michael Williams, Stephen P. Arneric. Cholinergic Therapies in Senile Dementia of Alzheimer Type
(SDAT), Danish Society of Pharmacology and Toxicology. March 22, 1996.
20.
Pharmacokinetic and safety studies on ABT-089; an orally active cholinergic channel modulator. J. E.
Campell, J. P. Sullivan, W. Arnold, Y. He, M. W. Holladay, Nan-Horng Lin, J. Daanen, Y. Li, K. C.
Marsh, B. Peterson, H. Nellans, J. Trivedi, S. P. Arneric. 1996, Abstract of papers of the Society for
Neuroscience, 25: 502.13
21.
ABT-089: A potent and selective cholinergic channel modulator with neuroprotective properties. J. P.
Sullivan, D. J. Anderson, C.A. Brigg, J. E. Campbell, D. Donnelly-Roberts, M. Gopalakrishnan, D.
Gunn, Y. He, M. W. Holladay, D. McKenna, N.-H. Lin, E. Molinari, M. Piattoni-Kaplan, I. Xue, M.
Williams, S. P. Arneric. 1996, Abstract of papers of the Society for Neuroscience, 25: 502.12
22.
Structural-Activity Relationships of Cholinergic Channel Modulators As Potential Treatments of
Alzheimer's Disease. Mark W Holladay, Nan-Horng Lin, James P. Sullivan, Michael W. Decker,
Stephen P. Arneric. 13th Meeting of the Medicinal Chemistry Division of Italian Chemical Society.
Paestum, Salero, September, 1996.
11
23.
Structure-Activity Studies On A Novel Series of Cholinergic Channel Activators Based On A
Heteroayl Ether Framework. Nan-Horng Lin, Melwyn A. Abreo, David E. Gunn, Suzanne A. Lebold,
Edmund Lee, James T. Wasicak, Ann-Marie Hettinger, David S. Garvey, Mark W. Holladay, David J.
Anderson, Jeffrey E. Campell, James P. Sullivan, Michael Williams, Stephen P. Arneric. 1996, Abstract
of papers of the American Chemical Society, 212: 078-Med.
24
Effect of ABT-089, A Novel Cholinergic Channel Modulator, On Cognitive Performance In Rats and
Monkeys. M. W. Decker, A. W. Bannon, P. Curzon, K. L. Gunther, J. D. Brioni, M. W. Holladay, N.-H.
Lin, Y. Li, J. Daanen, J. J. Buccafusco, M. A. Prendergast, W. J. Johnson and S. P.. Arneric. 1996,
Abstract of papers of the Society for Neuroscience, 25: 502.10
25.
Synthesis And Structure-Activity Relationships of Pyridine-Modified Analogs of 3-[2-(S)pyrrolidyl)methyl]oxy]pyridine, A-84543, A Potent Cholinergic Channel Modulator Nan-Horng Lin,
David E. Gunn, Yihong Li, Yun He, Hao Bai, Keith B. Ryther, Diana L. Donnelly-Roberts, David J.
Anderson, Jeffrey E. Campbell, James P. Sullivan, Stephen P. Arneric and Mark W. Holladay. 1997,
Abstract of papers of the American Chemical Society, 213: 044-Med.
26.
Synthesis And Structure-Activity Relationships of 5-Substituted Pyridine Analogs of 3-[2-((S)pyrrolidinyl)methoxy]pyridine, A-84543, A Potent Cholinergic Channel Modulator. Nan-Horng Lin,
Yihong Li, Yun He, Theresa Kuntzweiler, Diana L. Donnelly-Roberts, David J. Anderson, Jeffrey E.
Campbell, Stephen P. Arneric and Mark W. Holladay. 1997, Abstract of papers of the American
Chemical Society, 214: 008-Med.
27.
Identification, Initial Pharmacological Evaluation, and Structural-Activity Relationships of ABT-594 as
a Potent Orally Active Analgesic Agent Acting via Neuronal Nicotinic cetylcholine Receptors. M. W.
Hollada, J.T. Wasicak, Nan-Horng Lin, Y. He, K.R. Reyther, A.W. Bannon, M.J. Buckley, D.J.B. Kim,
M.W. Decker, D.J. Anderson, J.E. Campbell, D.L. Donnelly-Roberts, C.A. Briggs, D.G. Mckenna, W.E.
Niforatos, M. Piatoni-Kaplan, M.W. Williams, S.P. Arneric. 1997, Abstract of papers of the Society for
Neuroscience, 23: 477.6.
28.
Antinociceptive Effects of The Novel Neuronal Nicotinic Acetylcholine Receptor Agonist, ABT-594, in
Mice. Michael W. Decker, Anthony W. Bannon, Michael J. Buckley, David J. B. Kim, Mark W.
Holladay, Keith B. Ryther, Nan-Horng Lin, James T. Wasicak, Michael Williams, and Stephen P.
Arneric. 1997, Abstract of papers of the Society for Neuroscience, 23: 477.8.
29.
Synthesis and Structure-Activity Relationships of the 6-Chloro-5-Substituted Analogs of 3-[2-(S)pyrrolidinyl)-methoxy)pyridine, A-84543, A Potent Cholinergic Channel Activator. Yihong Li, NanHorng Lin, Frank Wagenaar, Edmond Lee, Yun He, Theresa Kuntzweiler, David J. Anderson, Stephen
P. Arneric, Mark W. Holladay. 1998, Abstract of papers of the American Chemical Society, 216: 146Med.
30.
Pyridyl Ether nicotic Acetylcholine Receptor Modulators with Potent Analgesic Activity. Mark W.
Holladay, James T. Wasicak, Nan-Horng Lin, Mick J. Dart, Keith B Ryther,. Yun He, Yihong Li, Hao
Bai, Curt B. Johnson, John F. Kincaid, Ferry F. Dannen, Ann-Mary Hettinger, Suzan A. Lebold,
Anthony W. Bannon, Michael W. Decker, Theresa A. Kuntzweiler, Diana L. Donnelly-Roberts, Clark A.
Briggs, Michael Williams, Stephen P. Arneric. 1998, Abstract of papers of the American Chemical
Society, 216: 206-Med.
31.
Synthesis and Structure-Activity Relationships of Pyrrolidine-Modified Analogs of 3-[2-(S)pyrrolidinyl)-methoxy)pyridine, A-84543, A Potent Cholinergic Channel Activator. Nan-Horng Lin,
Yihong Li, Yun He, Theresa Kuntzweiler, David J. Anderson, Mark W. Holladay, James P. Sullivan,
Stephen P. Arneric. 1998, Abstract of papers of the American Chemical Society, 216: 132-Med
32.
Identification of A Potent and Novel Nicotinic Receptor Ligand. Nan-Horng Lin, Monte Jade Science
& Technology Association of New England. November, 1999, Abstract of papers, p11.
12
33.
Synthesis and Biological Evaluation of Pyridine-Modified Analogs of 3-(2-Aminoethoxy)pyridine as
Novel Nicotinic Receptor Agonists. Nan-Horng Lin, Liming Dong, William Bunnel, David J.
Anderson,. Michael Meyer. 2001, Abstract of papers of the American Chemical Society, 221-Med
34.
Evaluation of PET Radioligands for the Neuronal Nicotinic Acetycoline Receptor. Roland
Schoenbachler, Katja Printz, Marianne F. Meyer, Michael Honer, Margarete Arras, Nan-Horng Lin,
Gerritt Westera. 12th Intl Symp on Radiopharmacology in Interlaken. June, 2001
35.
Design, synthesis, and biological activity of 4-[(4-cyano-2-aryl-benzyloxy)-(3-methyl-3H-imidazol-4yl)-methyl]-benzonitriles as potent, selective farnesyltransferase inhibitors. L. Wang, G. Wang, X.
Wang, Y. Tong, N. Leonard, G. Sullivan, Q. Li, J. Cohen, W. Gu, H. Zhang, J. Bauch, V. Stoll, K.
Marsh, S. Rosenberg, H. Sham, N. Lin. 2002, Abstract of papers of the American Chemical Society,
127-Med
36.
Discovery of potent and orally active farnesyltransferase inhibitors. Y. Tong, L. Wang, L. Hasvold, N.
Leonard, T. Li, Q. Li, W. Wang, J. Cohen, W. Gu, H. Zhang, J. Bauch, K. Marsh, S. H. Rosenberg, N.
Lin, H. L. Sham. 2002, Abstract of papers of the American Chemical Society, 129-Med.
37.
Lead optimization of imidazole-containing inhibitors of farnesyltransferase. G. T. Wang, X. Wang, D.
Park, G. Li, R. Gentles, L. Wang, N. Lin, G. Sullivan, J. Cohen, W. Gu, H. Zhang, J. Bauch, V. Stoll, K.
Marsh, S. Muchmore, S. H. Rosenberg, T. Sowin, H. L. Sham. 2002, Abstract of papers of the
American Chemical Society, 130-Med.
38.
Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)prop-2-ynyl]-1-yl-bezonitrile as novel farnesyl transferase inhibitors. N. Lin, L. Wang, J. Cohen, W. Gu,
D. Frost, H. Zhang, S. Rosenberg, H. L. Sham. 2002, Abstract of papers of the American Chemical
Society, 131-Med.
39.
Design and Synthesis of Pyridone Farnesyltransferase Inhibitors. Hasvold, Lisa A.; Wang, Weibo;
Rockway, Todd W.; Gwaltney, Stephen L., II; Nelson, Lissa T. J.; Mantei, Robert; Fakhoury, Stephen;
Sullivan, Gerard; Wang, Le; Lin, Nan-Horng; Li, Qun; Cohen, Jerry; Gu, Wen-Zhen; Zhang, Haiying;
Marsh, Kennan; Bauch, Joy; Gintant, Gary; McDermott, Jeff; Salmen, Heinz; Rosenberg, Saul; Sham,
Hing. 2002, Abstract of papers of the American Chemical Society, 126-Med.
40.
The effect of A-409100, a potent and highly selective farnesyl transferase inhibitor in vitro and in
vivo.Wen-Zhen Gu, Ingrid Joseph, Yi-Chun Wang, David Frost, Gerard Sullivan, Le Wang, Nan-Horng
Lin, Vincent Stoll, Mark Anderson, Paul Kroeger, Kennan Marsh, Shichung Ng, Saul Rosenberg, Hing
Sham, Haiying Zhang. 2003, Abstract of papers of the American Association for Cancer Research, 6186.
41.
Pyrazyl phenyl ureas as potent and selective Chk 1 inhibitors: The exploration of C6-position of pyrazyl
ring and SAR studies at C4-position of phenyl ring. Tao, Zhi-Fu; Li, Gaoquan; Wang, Gary T.; Kovar,
Peter; Zhang, Haiying; Park, Chang; Stewart, Kent; Sham, Hing L.; Sowin, Thomas; Rosenberg, Saul
H.; Lin, Nan-Horng. Abstracts of Papers, 229th ACS National Meeting, San Diego, CA, United States,
March 13-17, 2005, MEDI-145.
42.
Synthesis and biological evaluation of 3-Ethylidene-1,3-dihydro-indol-2-one as novel checkpoint 1
kinase inhibitors. Lin, Nan-Horng; Xia, Ping; Kovar, Peter; Park, Chang; Chen, Zehan; Zhang, Haiying;
Rosenberg, Saul; Sham, Hing L. Abstracts of Papers, 229th ACS National Meeting, San Diego, CA,
United States, March 13-17, 2005, MEDI-146.
43.
Structure-based design, synthesis and biological evaluation of macrocyclic Chk1 Inhibitors. Tao, ZhiFu; Wang, Le; Tong, Yunsong; Li, Gaoquan; Przytulinska, Magdalena; Sullivan, Gerard; Chen, Zehan;
Xiao, Zhan; Gu, Wendy; Xue, John; Bui, Mai-Ha; Merta, Philip; Kovar, Peter; Zhang, Haiying; Park,
Chang; Stewart, Kent D.; Sham, Hing L.; Sowin, Thomas; Rosenberg, Saul H.; Lin, Nan-Horng.
13
Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006,
MEDI-128.
44.
45.
Discovery of tricyclic pyrazoles as potent checkpoint-1 kinase inhibitors. Tong, Yunsong; Claiborne,
Akiyo; Tao, Zhi-Fu; Kovar, Peter; Park, Chang; Chen, Zehan; Credo, R. Bruce; Stewart, Kent D.;
Zhang, Haiying; Rosenberg, Saul; Sham, Hing L.; Sowin, Thomas; Lin, Nan-Horng. Abstracts of
Papers, 232nd ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006, MEDI-126.
The discovery of ABT-100, a potent and novel farnesyl transferase inhibitor. Nan-Horng Lin.
National Chung-Hsing University, invitation lecture, October, 2006.
46.
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one based
potent, and selective Chk-1 inhibitors. Wang, Le; Sullivan, Gerard M.; Hexamer, Laura; Hasvold, Lisa
A.; Thalji, Reema; Przytulinska, Magdalena; Tao, Zhi-Fu; Li, Gaoquan; Chen, Zehan; Xiao, Zhan; Gu,
Wen-Zhen; Xue, John; Hui, Mai-Ha; Metra, Philip; Kovar, Peter; Zhang, Haiying; Park, Chang; Stewart,
Kent; Sham, Hing; Sowin, Thomas; Rosenberg, Saul; Lin, Nan-Horng. Abstracts of Papers, 232nd
ACS National Meeting, San Francisco, CA, United States, Sept. 10-14, 2006, MEDI-125.
47.
The process of drug discovery. Nan-Horng Lin. National Chung-Hsing University, invitation lecture,
January 3, 2007
48.
Investigation of novel 7,8-disubstituted-5, 10-dihydro-dibenzo[b, e][1,4]diazepin-11-ones as potent and
selective Chk1 inhibitors. L. A. Hasvold, L. Wang, G. M. Sullivan, M. Przytulinska, L. Hexamer, Z.
Xiao, Z. Chen, W-G. Gu, P. Merta, J. Xue, P. Kovar, H. Zhang, J. Bouska, C. Park, T. Sowin, S.
Rosenberg, N-H. Lin. Abstracts of Papers, 233rd ACS National Meeting, Chicago, United States, Mar.
25-28, 2007, MEDI-122.
49.
Investigation of novel 7substituted and 8-substituted -5, 10-dihydro-dibenzo[b, e][1,4]diazepin-11-ones
based potent, and selective Chk1 inhibitors. L. Hexamer, L. Wang, G. M. Sullivan, M. Przytulinska, Z.
Xiao, Z. Chen, W-G. Gu, M-H. Bui, P. Merta, J. Xue, P. Kovar, H. Zhang, K.C. Marsh, T. Sowin, S.
Rosenberg, N-H. Lin. Abstracts of Papers, 233rd ACS National Meeting, Chicago, United States, Mar.
25-28, 2007, MEDI-123.
50.
Integrated Biology and Chemistry Service in China at Medicilon. Nan-Horng Lin, The 11th Shanghai
International Forum on Biotechnology & Pharmaceutical Industry. Shanghai, China, June 1-3, 2009,
PUBLICATIONS
1.
-hydroxydeoxocryptojaponol. YehHsiung Kuo, Nan-Horng Lin and Yao-Tung Lin. J. Chin. Chem. Soc., 1980, 27, 19.
2.
Total synthesis of (+)-12,14-difluoro-prostaglandin F2alpha. Nan-Horng Lin, Paul A. Grieco. Fifth
Semester Report, Indiana University, June, 1981.
3.
Macrolide antibiotics: chemical transformation in the tylosin series. partial synthesis of tylonolide
hemiacetal. Paul A Grieco, Nan-Horng Lin and Junji Inanaga., J. Org. Chem., 1983, 48, 892.
14
4.
Bicyclo [2,2,1] heptane in organic synthesis. total synthesis of the sixteen membered ring macrolide
tylonolide hemiacetal: synthesis and coupling of the C (3) -C(9) and C(11) -C(17) fragments. Paul A
Grieco, Junji Inanaga, Nan-Horng Lin, Tesuji Yanami. J. Am. Chem. Soc., 1983, 104, 5781.
5.
Total synthesis of the sixteen membered ring macrolide tylonolide hemiacetal. Nan-Horng Lin, Diss.
Abstr. Int. B 1984, 44, 3083.
6.
Enantioselective total synthesis of (+)-pumiliotoxin A. Nan-Horng Lin, Larry E. Overman. J. Org.
Chem., 1985, 50, 3669.
7.
Novel leukotriene antagonists. Nan-Horng Lin. MOI 14105, Miles Inc, 1987.
8.
Tetrazolium salts and their use in diagnostic test. Robert P. Hatch, Nan-Horng Lin and Jurgen Kocher.
MOI 14431, Miles Inc, 1989.
9.
Synthesis and evaluation of nicotine analogs as neural cholinergic channel receptor ligands. Nan-Horng
Lin, David J. Anderson and George Carrera. J. Med. Chem., 1994, 37, 3542-3553.
10.
Studies on the isoxazole formation from alkyl carboxylic esters. Nan-Horng Lin and Yun He. Synthesis.
1994, 989-992.
11.
Synthesis and structure-activity relationships of pyrrolidine-modified analogs of the potent cholinergic
channel activator, ABT 418. Nan-Horng Lin, Yun He, David J Anderson, James T. Wasicak, Richard
Kasson, David Sweeny and James P. Sullivan. Biorg. & Med. Chem.Lett. 1994, 4, 2389-2394.
12.
Synthesis and in vitro evaluation of alkylamino heterocyclic ethers as nicotinic receptor ligands. NanHorng Lin, Suzanne A. Lebold, Melwyn Abreo, David J. Anderson, James Sullivan, Stephen P. Arneric.
Biorg. & Med. Chem. Lett. 1994, 4, 3112-3116.
13.
Ligands for brain cholinergic channel receptors: synthesis and in vitro characterization of novel
isoxazoles and isothiazoles as bioisosteric replacements pyridine ring in nicotine. David S. Garvey,
James T. Wasicak, Richard L. Elliott, Suzanne Lebold, Ann-Marie Hettinger, George M. Carrera, NanHorng Lin, Yun He, Mark W.Holladay, David J. Anderson, Evelyn D. Cadman, Joanna L. Raszkiewicz,
James P. Sullivan, and Stephen P. Arneric. J. Med. Chem. 1994, 37, 4455-4463.
14.
A short, efficient synthesis of the novel cholinergic channel activator, ABT 418, from L-pyroglutamic
acid. Nan-Horng Lin, Yun He and Hana Kopecka. Tetrahedron Lett. 1995, 36, 2563-2566.
15.
A short , efficient synthesis of the novel cholinergic channel agonist, ABT 418, from L-Proline. Richard
L. Elliott, Hana Kopecka, Nan-Horng Lin, Yun He and David S. Garvey. Synthesis. 1995, 772-774.
16.
Synthesis and structure-activity relationships of 2'-(R) and (S)-pyrrolidine-modified analogs of the
cholinergic channel activator, ABT 418. Nan-Horng Lin, Yun He, Stephen P. Arneric and James P.
Sullivan. Bioorg. & Med. Chem. Letters. 1995, 5, 1141-1146.
17.
Structure-activity relationships of nicotinic acetylcholine receptor agonists as potential treatments for
dementia. Mark W. Holladay, Suzanne A.Lebold, Nan-Horng Lin. Drug Development Res. 1995, 35,
191-213.
18.
Synthetic and pharmacological studies on the neurotoxic delphinium alkaloid methyllycacotine and
related compounds. John. M. Jacyno, Nan-Horng Lin, Mark W. Holladay, James P. Sullivan. Curr.
Top. Plant Physiol., 1995, 15, 294-296.
19.
Novel 3-pyridylethers with subnanomolar affinity for central nicotinic acetylcholine receptors. Melwyn
A Abreo, Nan-Horng Lin,* David S. Garvey, David E. Gunn, Anne-Marie Hettinger, Richard, L.
15
Elliott, Suzanne A. Lebold, Mark W. Holladay, David J. Anderson, Diana Donnelly-Roberts, James P.
Sullivan, Stephen P. Arneric and Michael Williams. J. Med. Chem. 1996, 39, 817-825.
20.
Synthetic and pharmacological studies on neurotoxic Delphinium alkaloids methyllycaconitine and
related compounds. John. M. Jacyno, Nan-Horng Lin, Mark W. Holladay, James P. Sullivan. (In):
Current Topics in Plant Physiology 15, (Phytochemicals and Health), 1995, 294-296
21.
2-(Aryloxymethyl) Azacyclic Analogs as Novel Nicotinic Acetylcholine Receptor (nAChR) Ligands.
Richard L. Elliott, Hana Kopecka, David E. Gunn, Nan-Horng Lin, David S. Garvey, Keith B. Ryther,
Mark W. Holladay, David J. Anderson, Jeffrey E. Campbell, Diana Donnelly-Roberts, Marietta PiattoniKaplan, James P. Sullivan, Michael J. Buckley, Karen L. Gunther, Alyssa O'Neill, Mike W Decker,
Stephen P. Arneric. Bioorg. & Med. Chem. Letters. 1996, 6, 2283-2288.
22.
Lycaconitine Revisited: Partial Synthesis and Neuronal Acetylcholine Receptor Affinities. J. M. Jacyno.
J. S. Harwood, Nan-Horng Lin, J. E. Campbell, J. P. Sullivan, M. W. Holladay. Journal of Natural
Product. 1996, 59, 707-709.
23.
Efficient Total Synthesis of Pumiliotoxins A and B. Applications of Iodide-Promoted Iminium IonAlkyne Cyclizations in Alkaloid Construction. Nan-Horng Lin, Larry E. Overman, Michael H.
Rabinowitz, Leslie A. Robinson, Matthew J. Sharp and Jeffrey Zablocki. J. Am. Chem. Soc. 1996, 118,
9062-9072.
24.
Quantitative Structure-Activity Relationships of Nicotine Analogues as Neuronal Nicotinic
Acetylcholine Receptor Ligands. Ki Hwan Kim, Nan-Horng Lin, David J. Anderson. J. Bioorganic &
Medicinal Chemistry , 1996, 4, 2211-2217
25.
ABT-089: orally An Orally Effective Cholinergic Channel Modulator With Potential With Cognition
Enhancing and Neuroprotective Activity. Stephen P. Arneric´, Bannon, A. W., Briggs, C.A., Brioni,
J.D., Bucaffusco, J.J., Decker, M.W., Gopalakrishan, M., Holladay, M.W., Kynel, J., Lin, N.H., Marsh,
K.C., Qui, Y.H., Radek, R., Donnelly-Roberts, D.L., Sullivan, J.P., Williams, M. in BekerR, Giacobini
E, Robert P (eds): Alzheimer Disease: From Molecular Biology to Therapy. Birkhauser Boston, pp 287292, 1996
26.
Progress in The Development of Potent and Selective Cholinergic Channel Modulators (ChCMs).
Holladay, Mark W.; Lin, Nan-Horng.; Sullivan, James P.; Donnelly-Roberts, Diana L.; Decker,
Michael W.; Brioni, Jorge D.; Ferreo, James L.; Rodrigues, A David.; Marsh, Kennan G.; Buccafusco,
Jerry J.; Arneric, Stephen P. Pharmacochem. Libr. 1997, 28, 127-136.
27.
Structure-Activity Studies on ABT-089 : An Orally Bioavailable 3-Pyridyl Ether Cholinergic Channel
Modulator With Cognitive Enhancing Properties. Nan-Horng Lin, David E. Gunn, Keith B. Ryther,
David S. Garvey, Diana L. Donnelly-Roberts, Michael W. Decker, Jorge D. Brioni, Michael J. Buckley,
A. David Rodrigues, Kennan G. Marsh, David J. Anderson, James P. Sullivan, Michael Williams,
Stephen P. Arneric, Mark W. Holladay. J. Med. Chem. 1997, 40, 385-390.
28
ABT-089[2-Methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: A Potent and Selective
Cholinergic Channel Modulator with Cytoprotective Properties. J. P. Sullivan, D. Donnelly-Roberts, C.
A. Brigg, M. Gopalakrishnan, I. Hu, J. E. Campbell, D.J. Anderson, M. Piatton-Kaplan, E. Molinari, D.
G. McKenna, D. E. Gunn, Nan-Horng Lin, K. B. Ryther, Y. He, M. W. Holladay, M. Williams, S. P.
Arneric. J. Pharmacol. Exp. Ther. 1997, 283,235-246.
29.
ABT-089 [2-methyl-3-(2-(s)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A Novel Cholinergic
Channel Modulator with effects on Cognitive Performance in Rats and Monkeys. Michael W. Decker,
Anthony W. Bannon, Peter Curzon, Karen L. Gunther, Jorge D. Brioni, Mark W. Holladay, Nan-Horng
16
Lin Yihong Li, Jerome F. Daanen, Jerry J. Buccafusco, Mark A. Prendergast, William J. Jackson, and
Stephen P. Arneric´. J. Pharmacol. Exp. Ther. 1997, 283, 247-258.
30.
ABT-089 [2-methyl-3-(2-(s)-pyrrolidinylmethoxy)pyridine dihydrochloride]: An Orally Effective
Cholinergic Channel Modulator With Potential Once-a-Day Dosing and Cardiovascular Safety. Stephen
P. Arneric´, Jeffrey E. Campell, Sherry Carroll, Jerome F. Daanen, Mark W. Holladay, P. Johnson, NanHorng Lin, Kennan C. Marsch, Bud Peterson, Yihong Qui, Ellen Roberts, A. David Rodrigues, James
P. Sullivan, Jay Trivedi and Michael Williams. Drug. Dev. Res. 1997, 41, 31-43.
31.
Identification and Structure-Activity Relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine
(ABT-594), a Potent, Orally Active Non-opiate Analgesic Agent Acting via Neuronal Nicotinic
Acetylcholine Receptors. Mark W. Holladay, James T. Wasicak, Nan-Horng Lin, Yun He, Keith B.
Ryther, Anthony W. Bannon, Michael J. Buckley, David J. B. Kim, Michael W. Decker, David J.
Anderson, Jeffrey E. Campbell, Theresa A. Kuntzweiler, Diana L. Donnelly-Roberts, Marietta PiattoniKaplan, Clark A. Briggs, Michael Williams, Stephen P. Arneric. J. Med. Chem. 1998, 41, 407-412
32.
Synthesis And Structure-Activity Relationships of Pyridine-Modified Analogs of 3-[[2-((S)pyrrolidyl)methyl]oxy]pyridine, A-84543, A Potent Cholinergic Channel Modulator Nan-Horng Lin,
David E. Gunn, Yihong Li, Yun He, Hao Bai, Keith B. Ryther, Diana L. Donnelly-Roberts, David J.
Anderson, Jeffrey E. Campbell, James P. Sullivan, Stephen P. Arneric and Mark W. Holladay. Bioorg. &
Med.Chem. Lett., 1998, 8, 249-254.
33.
"Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in
mice. Michael W. Decker, Anthony W. Bannon, Michael J. Buckley, David J. B. Kim, Mark W.
Holladay, Keith B. Ryther, Nan-Horng Lin, James T. Wasicak, Michael Williams, and Stephen P.
Arneric. Eur. J. Pharmacol. 1998. 346,23-33.
34.
5-((2R)-Azetidinylmethoxy)-2-chloropyridine [ABT-594]: A Novel Orally Effective Antinociceptive
Agent Acting via Neuronal Nicotinic Acetylcholine Receptors. II. In vivo Characterization. A. W.
Bannon, M. W. Decker, P. Curzon, M. J. Buckley, D. B. J.Kim, J. K. Lynch, J. T. Wasicak, Nan-Horng
Lin , W. H. Arnold, M. W. Holladay and S. P. Arneric. J. Pharmacol. Exp. Therap. 1998, 285, 787794.
35.
Recent Developments in Neuronal Nicotinic Acetylcholine Receptor (nAChR) Modulators. Nan-Horng
Lin and Michael D. Meyer. Expert Opin. Ther. Pat. 1998, 8(8), 991-1015.
36
Structureactivity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and
azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in
mice. M. W. Holladay, H. Bai, Y. Li, N.-H. Lin, J. F. Daanen, K. B. Ryther, J. T. Wasicak, J. F.
Kincaid, Y. He, A.-M.Hettinger, P. Huang, D. J. Anderson, A. W. Bannon, M. J. Buckley, J. E.
Campbell, D. L. Donnelly-Roberts, K. L. Gunther, D. J. B. Kim, T. A. Kuntzweiler, J. P. Sullivan, M.
W. Decker, S. P. Arneric. Bioorg. & Med. Chem. Lett. 1998, 8, 2797-2803.
37
Structure-Activity Studies On A Novel Series of Cholinergic Channel Activators Based On a Heteroaryl
Ether Framework.. Nan-Horng Lin, Suzanne A. Lebold, Melwyn Abreo, David J. Anderson, James
Sullivan, Stephen P. Arneric. Bioorg & Med. Chem. Lett. 1999, 9(18), 2747-2752.
38
Synthesis And Structure-Activity Relationships of 5-Substituted Pyridien Of 3-[2-((S)pyrrolidinyl)methoxy]pyridine, A-84543, A Potent Cholinergic Channel Modulator. Nan-Horng Lin,
Yihong Li, Yun He, Mark W. Holladay, Theresa Kuntzweiler, David J. Anderson, Jeffrey E. Campbell,
Stephen P. Arneric. Bioorg & Med. Chem. Lett. 2001, 11, 631-633.
39.
Synthesis And Biological Evaluation of Pyridine-Modified Analogs of 3-(2-Aminoethoxy)pyridine As
Novel Nicotinic Receptor Ligands. Nan-Horng Lin, Liming Dong, William H. Bunnelle, David J.
Anderson and Michael D. Meyer. Bioorg & Med. Chem. Lett. 2002, 12, 3321-3324.
17
40.
Synthesis And Biological Evaluation of 4-[3-biphenyl-2-yl-1hydroxy-1-(3-methyl-3-H-imidazo-4yl)prop-2-ynyl]-1-yl-bezonitrile as Noval Farnesyltrasferase Inhibitor. Nan-Horng Lin, Le Wang, Jerry
Cohen, Wen-Zhen Gu, David Frost, Haaiing Zhang, Saul Rosenberg and Hing Sham. Bioorg & Med.
Chem. Lett. 2003, 13, 1293-1296.
41.
Discovery of Potent Imidazole And Cyanophenyl Containing Farnesyltransferase Inhibitors With
Improved Oral Bbioavailability. Tong, Yunsong; Lin, Nan-Horng; Wang, Le; Hasvold, Lisa; Wang,
Weibo; Leonard, Nicholas; Li, Tongmei; Li, Qun; Cohen, Jerry; Gu, Wen-Zhen; Zhang, Haiying; Stoll,
Vincent; Bauch, Joy; Marsh, Kennan; Rosenberg, Saul H.; Sham, Hing L. Bioorg & Med. Chem. Lett.
2003, 13, 1571-1574.
42.
Design and Synthesis of Pyridone Farnesyltransferase Inhibitors. Hasvold, Lisa A.; Wang, Weibo;
Rockway, Todd W.; Gwaltney, Stephen L., II; Nelson, Lissa T. J.; Mantei, Robert; Fakhoury, Stephen;
Sullivan, Gerard; Wang, Le; Lin, Nan-Horng; Li, Qun; Cohen, Jerry; Gu, Wen-Zhen; Zhang, Haiying;
Marsh, Kennan; Bauch, Joy; Gintant, Gary; McDermott, Jeff; Salmen, Heinz; Rosenberg, Saul; Sham,
Hing. Bioorg & Med. Chem. Lett. 2003, 4001-4005.
43.
Synthesis And Biological Evaluation of 4-[(3-Methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)methyl]-benzonitrile as Noval Farnesyltrasferase Inhibitor. Nan-Horng Lin, Le Wang, Jerry Cohen,
Wen-Zhen Gu, David Frost, Haiying Zhang, Saul Rosenberg and Hing Sham. Bioorg & Med. Chem.
Lett. 2003, 13, 3821-3825.
44.
Design, Synthesis, and Biological Activity of 4-[(4-Cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4yl)methyl]benzonitriles as Potent and Selective Farnesyltransferase Inhibitors. Wang, L.; Wang, G. T.;
Wang, X.; Tong, Y.; Sullivan, G.; Park, D.; Leonard, N. M.; Li, Q.; Cohen, J.; Gu, W.-Z.; Zhang, H.;
Bauch, J. L.; Jakob, C. G.; Hutchins, C. W.; Stoll, V. S.; Marsh, K.; Rosenberg, S. H.; Sham, H. L.; Lin,
N.-H.; J. Med. Chem., 2004, 47, 612.
45.
Synthesis of 1H-Pyridin-2-one Derivative as Potent and Selective Farnesyltransferase Inhibitors. Wang,
Le.; Nan-Horng Lin, Qun Li, Rodger F. Henry, Haiying Zhang, Jerome Cohen, Wen-Zhen Gu, Kennan
Marsh, Joy Bauch, Saul Rosenberg, Hing L. Sham. Bioorg & Med. Chem. Lett. 2004, 14, 4603-4606.
46.
ABT-089: Pharmacological Properties of a Neuronal Nicotinic Acetylcholine Receptor Agonist for the
Potential Treatment of Cognitive Disorders. Lynne E. Reuter, David J. Anderson, Clark A. Briggs, Diana
L. Donnelly-Roberts, Gary A. Gintant, Murari Gopalakrishnan, Nan-Horng Lin, Mark A. Osinski,
Glenn A. Reinhart, Michael J. Buckley, Ruth L. Martin, Jeffrey S. McDermott, Lee C. Preusser, Terese
R. Seifert, Zhi Su, Bryan Cox, Michael W. Decker, and James P. Sullivan. CNS Drug Reviews. 2004, 10,
167-182.
47.
Synthesis And Biological Evaluation of 1-Benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole As Novel
Farnesyltransferase Inhibitor. Nan-Horng Lin, Le Wang, Xilu Wang, Gary T. Wang, Jerry Cohen, WenZhen Gu, Haiying Zhang, Saul Rosenberg and Hing L. Sham. Bioorg & Med. Chem. Lett. 2004, 14(20),
5057-5062
48.
Design, Synthesis and Activity of Achiral Analogs of 2-Quinolones and Related Compounds as NonThiol Farnesyltransferase Inhibitors. Qun Li, Nan-Horng Lin, Keith W. Woods, Akiyo Claiborne,
Weibo Wang, Wendy Gu, Jerry Cohen, Vincent Stoll and Hing L. Sham. Bioorg & Med. Chem. Lett.
2005, 15, 2033-2039.
49.
A-432411, a novel indolinone compound that disrupts spindle pole formation and inhibits human cancer
cell growth. Zehan Chen, Philip J. Merta, Nan-Hong Lin, Stephen K. Tahir, Peter Kovar, Hing Sham,
and Haiying Zhang. Mol. Cancer Ther. 2005, 4, 562-568.
50.
Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, pro-apoptotic and anti-angiogenic effects in xenograft models. Debra Ferguson, Luis E.
18
Rodriguez, Joann P. Palma, Marion Refici, Kenneth Jarvis, Jacqueline O’Connor, Gerard M. Sullivan,
David Frost, Kennan Marsh, Joy Bauch, Haiying Zhang, Nan-Horng Lin, Saul Rosenberg, Hing L.
Sham, Ingrid B.J.K. Joseph. Clinical. Cancer Res., 2005, 11, 3045-3054.
51.
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyano- pyrazi-2-yl)ureas as Potent and Selective Inhibitors of Chk1
Kinase: Synthesis, Preliminary SAR, and Biological Activities. Wang, Gary T.; Li, Gaoquan; Mantei,
Robert A.; Chen, Zehan; Kovar, Peter; Gu, Wendy; Xiao, Zhan; Zhang, Haiying; Sham, Hing L.; Sowin,
Thomas; Rosenberg, Saul H.; Lin, Nan-Horng. J. Med. Chem., 2005, 48, 3118-3121.
52.
A facile synthesis of antitumoral indeno[1,2-c]pyrazole-4-one by mild oxidation with molecular oxygen.
Tao, Zhi-Fu; Sowin, Thomas J.; Lin, Nan-Horng. Tetrahedron Lett. 2005, 46(44), 7615-7618.
53.
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies. Gu, WenZhen; Joseph, Ingrid; Wang, Yi-Chun; Frost, David; Sullivan, Gerard M.; Wang, Le; Lin, Nan-Horng;
Cohen, Jerry; Stoll, Vincent S.; Jakob, Clarissa G.; Muchmore, Steven W.; Harlan, John E.; Holzman,
Tom; Walten, Karl A.; Ladror, Uri S.; Anderson, Mark G.; Kroeger, Paul; Rodriguez, Luis E.; Jarvis,
Kenneth P.; Ferguson, Debra; Marsh, Kennan; Ng, Shichung; Rosenberg, Saul H.; Sham, Hing L.;
Zhang, Haiying. Anti-Cancer Drugs., 2005, 16, 1059-1069.
54.
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1
inhibitors. Nan-Horng Lin, Ping Xia, Peter Kovar, Chang Park, Zehan Chen, Haiying Zhang, Saul H.
Rosenberg and Hing L. Sham. Bioorg & Med. Chem. Lett. 2006, 16, 421-426.
55.
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as
potent Chk1 kinase inhibitors. Li, Gaoquan; Hasvold, Lisa A.; Tao, Zhi-Fu; Wang, Gary T.; Gwaltney,
Stephen L.; Patel, Jyoti; Kovar, Peter; Credo, Robert B.; Chen, Zehan; Zhang, Haiying; Park, Chang;
Sham, Hing L.; Sowin, Thomas; Rosenberg, Saul H.; Lin, Nan-Horng. Bioorg & Med. Chem. Lett.
2006, 16, 2293-2298.
56.
Chk1 inhibitors for novel cancer treatment. Tao, Zhi-Fu; Lin, Nan-Horng. Anti-Cancer Agents in
Medicinal Chemistry, 2006, 6(4), 377-388.
57.
Selective Chk1 inhibitors differentially sensitize p53-deficient cancer cells to cancer therapeutics. Chen,
Zehan; Xiao, Zhan; Gu, Wen-zhen; Xue, John; Bui, Mai H.; Kovar, Peter; Li, Gaoquan; Wang, Gary;
Tao, Zhi-Fu; Tong, Yunsong; Lin, Nan-Horng; Sham, Hing L.; Wang, Jean Y. J.; Sowin, Thomas J.;
Rosenberg, Saul H.; Zhang, Haiying. International Journal of Cancer, 2006, 119(12), 2784-2794.
58.
Structure-Based Design, Synthesis, and Biological Evaluation of Potent and Selective Macrocyclic
Checkpoint Kinase 1 Inhibitors. Zhi-Fu Tao, Le Wang, Kent D. Stewart, Zehan Chen, Wendy Gu, MaiHa Bui, Philip Merta, Haiying Zhang, Peter Kovar, Eric Johnson, Chang Park, Russell Judge, Saul
Rosenberg, Thomas Sowin, and Nan-Horng Lin. J. Med. Chem., 2007, 50 (7), 1514 –1527.
59.
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint
kinase 1 inhibitors. Yunsong Tong, Akiyo Claiborne, Kent D. Stewart, Chang Park, Peter Kovar, Zehan
Chen, Robert B. Credo, Wen-Zhen Gu, Stephen L. Gwaltney II, Russell A. Judge, Haiying Zhang, Tom
Sowin and Nan-Horng Lin. Bioorg & Med. Chem. 2007, 16 (7), 2759-2767.
60.
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: Extended exploration on
phenyl ring substitutions and preliminary ADME/PK studies. Yunsong Tong, Akiyo Claiborne,
Magdalena Pyzytulinska, Zhi-Fu Tao, Kent D. Stewart, Peter Kovar, Zehan Chen, Robert B. Credo, Ran
Guan, Philip J. Merta, Haiying Zhang, Jennifer Bouska, Elizabeth A. Everitt, Bernard P. Murry, Dean
Hickman, Tim J. Stratton, Jian Wu, Saul H. Rosenberg, Hing L. Sham, Thomas J. Sowin and NanHorng Lin. Bioorg & Med. Chem. Lett. 2007, 3618-3623.
19
61.
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent
and selective Chk-1 inhibitors. Le Wang, Gerard M. Sullivan, Laura A. Hexamer, Lisa A. Hasvold,
Reema Thalji, Magdalena Przytulinska, Zhi-Fu Tao, Gaoquan Li, Zehan Chen, Zhan Xiao, Wen-Zhen
Gu, John Xue, Mai-Ha Bui, Philip Merta, Peter Kovar, Jennifer J. Bouska, Haiying Zhang, Chang Park,
Kent D. Stewart, Hing L. Sham, Thomas J. Sowin, Saul H. Rosenberg, and Nan-Horng Lin. J. Med.
Chem., 2007, 50 (7), 4162-4176..
62.
Synthesis and biological evaluation of 4′-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)biphenyl-4-ol as potent Chk1 inhibitors. Zhi-Fu Tao, Gaoquan Li, Yunsong Tong, Zehan Chen, Philip
Merta, Peter Kovar, Haiying Zhang, Saul H. Rosenberg, Hing L. Sham, Thomas J. Sowin and NanHorng Lin. Bioorg & Med. Chem. Lett. 2007, 4308-4315.
63.
Discovery of 4′-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4′-(1,4-dihydro-indeno[1,2c]pyrazol-3-yl)-pyridine-2′-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors. Zhi-Fu Tao,
Gaoquan Li, Yunsong Tong, Kent D. Stewart, Zehan Chen, Mai-Ha Bui, Philip Merta, Chang Park, Peter
Kovar, Haiying Zhang, Hing L. Sham, Thomas J. Sowin, Saul H. Rosenberg, and Nan-Horng Lin.
Bioorg & Med. Chem. Lett. 2007, 5944-5951.
64.
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors. Gaoquan Li, Zhi-Fu Tao,
Yunsong Tong, Magdalena K. Przytulinska, Peter Kovar, Philip Merta, Zehan Chen, Haiying Zhang,
Thomas Sowin, Saul H. Rosenberg, Nan-Horng Lin. Bioorg & Med. Chem. Lett. 2007, 6499-6504.
65.
Macrocyclic ureas as potent and selective Chk1 inhibitors: An improved synthesis, kinome profiling,
structure–activity relationships, and preliminary pharmacokinetics. Zhi-Fu Tao, Zehan Chen, Mai-Ha
Bui, Peter Kovar, Eric Johnson, Jennifer Bouska, Haiying Zhang, Saul Rosenberg, Thomas Sowin, NanHorng Lin. Bioorg & Med. Chem. Lett. 2007, 6593-6601.
66.
Synthesis of Macrocyclic Urea Kinase Inhibitors. Tao, Zhi-Fu; Sowin, Thomas J; Lin, Nan-Horng.
Synlett. Accounts and Rapid Communication in Synthetic Organic Chemistry, 2007, 18 (18), 2855-2858.
67.
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1
inhibitors. Lisa A Hasvold, Le Wang, Magdalena Przytulinska, Zhan Xiao, Zehan Chen, Wen-Zhen Gu,
Philip J Merta, John Xue, Peter Kovar, Haiying Zhang, Chang Park, Thomas J Sowin, Saul H
Rosenberg, Nan-Horng Lin. Bioorg & Med. Chem. Lett. 2008, 2311-2315.
68.
Cyclin B1 is an efficacy-predicting biomarker for Chk1 inhibitors. Zhan Xiao; John Xue; WeZhen Gu;
Mai Bui; Gaoquan Li; Zhi-Fu Tao; Nan-Horng Lin; Thomas J. Sowin ; Haiying Zhang. Biomarker,
Biomarker, 2008, 13 (6), 579-596.
69.
Discovery of 3H-Benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as Potent, Highly Selective, and Orally
Bioavailable Inhibitors of the Human Protooncogene Proviral Insertion Site in Moloney Murine
Leukemia Virus (PIM) Kinases. Tao, Zhi-Fu; Hasvold, Lisa A.; Leverson, Joel D.; Han, Edward K.;
Guan, Ran; Johnson, Eric F.; Stoll, Vincent S.; Stewart, Kent D.; Stamper, Geoff; Soni, Nirupama;
Bouska, Jennifer J.; Luo, Yan; Sowin, Thomas J.; Lin, Nan-Horng; Giranda, Vincent S.; Rosenberg,
Saul H.; Penning, Thomas D. J. Med. Chem. 52(21), 2009, 6621-6636..
20