CURRICULUM VITAE
Personal Details
Name, surname: Jan Korabecny
Date and place of birth: 31. 8. 1983/Pardubice
Nationality: Czech
Address: Hradek 13, 503 15, Czech Republic
Mobile No.: +420 724 770 956
E-mail address: korabecny.jan@gmail.com
Summary of Education
1997-2003
High school studies at Gymnazium Bozeny Nemcove, Hradec Kralove
2003-2008
MSc. studies at Faculty of Pharmacy in Hradec Kralove, Charles
University in Prague (diploma work titled: Synthesis of differently
substituted arylguanidines as potential drug candidates VI., supervisor:
Dr. Karel Palat)
10/2008-6/2012
Doctoral studies at Faculty of Pharmacy in Hradec Kralove (Charles
University in Prague), Department of Pharmaceutical Chemistry and
Drug Control in collaboration with Faculty of Military Health Sciences
(University of Defence), Department of Toxicology and Military
Pharmacy. Doctoral thesis titled: Synthesis of tetrahydroacridine based
acetylcholinesterase inhibitors (supervisors: assoc. prof. Veronika
Opletalova, prof. Kamil Kuca)
Work Experience
-
-
Since 9/2011 Academic worker at Department of Toxicology and Military Pharmacy
(Faculty of Military Health Sciences in Hradec Kralove, University of Defence in
Brno)
Since 5/2012 Academic worker at Center for Biomedical Research (University
Hospital in Hradec Kralove)
8/2012-6/2015
Post-doctoral studies at Center for Biomedical Research
(University Hospital in Hradec Kralove)
Since 5/2014 junior researcher at National Institute of Mental Health (Klecany,
Prague)
Work Profile
-
Experience in synthesis and handling of different organic compounds
-
Development of new agents with potential cholinergic, antitumor, anti-mycotic and
anti-tuberculotic activity
-
Molecular modeling studies and design of novel drugs
Abilities and other relevant details
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Driving license (group B)
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Computer knowledge operating system Microsoft Windows and Mac OS X
-
MS office (word, excel, power point, publisher)
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Programs used for drawing structures and for interpretation of NMR spectra Chemdraw, ChemSketch and ISIS draw, MestreNova, MestreC
-
Molecular docking software – PyMol viewer, Autodock Tools, Autodock Vina,
PoseView
Languages
French language (basic knowledge)
English language (STANAG 2 – 9/2012)
Achievements
2008 Award of Penta society for the best diploma thesis at the Department of inorganic and
organic chemistry (titled Synthesis of differently substituted arylguaindines as
potential drug candidates VI.)
2010 Honored by Czech Neuropsychopharmacological society for the best poster
presentation (authors, title: Korabecny, J.; Holas, O.; Musilek, K.; Opletalova, V.;
Pohanka, M.; Kuca, K. Newly prepared derivatives of 7-MEOTA. 52. Czech and
Slovak psychopharmacological conference, Lazne Jesenik (Czech republic) 6.10.1.2010, Supplementum 1, 2010, p. 45.)
2013 Honored by Czech Neuropsychopharmacological society for the best poster
presentation (authors, title: Hroudova, J.; Fisar Z., Raboch, J.; Korabecny, J.; Kuca, K.
In vitro účinky inhibitorů acetlycholinestráz na aktzivitu monoaminooxidáz a NADH
dehydrogenázy. 55. Czech and Slovak psychopharmacological conference, Lazne
Jesenik (Czech republic) 4.-8.1.2013, Supplementum 1, 2013, p. 65.)
2013 Best poster award (authors, title: Kuca, K.; Musilek, K.; Jun, D.; Zdarova-Karasova,
J.; Kunes, M.; Soukup, O.; Korabecny, O.; Sepsova, V.; Hrabinova, M. Novel
acetylcholinesterase reactivators – antidotes against nerve agents. International
Conference on Pharmacology and Drug Development Singapore (Singapore) 9. – 11.
12. 2013.)
2015 Best poster award (authors, title: Svobodova, L.; Nepovimova, E.; Korabecny, J.;
Kucerova-Chlupacova, M.; Kuca, K. Tacrine-Benzothiazole Hybrids - Novel
Multitarget Agents To Combat Alzheimer’s Disease. EPSA Annual Congress in
Toulouse, Science day (Toulouse, France) 30.3.2015
2015 Best publication award for 2014 in neuroscience research awarded by Czech
Alzheimer Society (Nepovimova, E.; Uliassi, E.; Korabecny, J.; Peña-Altamira, L.E.;
Samez, S.; Pesaresi, A.; Garcia, G.E.; Bartolini, M.; Andrisano, V.; Bergamini, C.;
Fato, R.; Lamba, D.; Roberti, M. Kuca, K.; Monti, B.; Bolognesi, M.L. Multitarget
drug design strategy: quinone-tacrine hybrids designed to block amyloid-beta
aggregation and to exert anticholinesterase and antioxidant effects. J. Med. Chem.
2014, 57, 8576 8589. IF = 5.480.)
Educational stay
4/2011-6/2011Three months internship in Kosice (Slovakia), synthesizing new
acetylcholinesterase inhibitors based on 7-methoxytacrine (supervisor Dr.
Hamulakova)
6/2013-7/2013Two months internship in Rouen (France), development of new
acetylcholinesterase reactivators (supervisors Dr. Ludovic Jean, prof. P. Y.
Renard)
4/2014-5/2014Two months internship in Daejeon (South Korea), drug design and synthesis of
novel acetylcholinesterase reactivators (supervisor Dr. Y.-S. Jung)
4/2015-6/2015two months internship in Würzburg (Germany), drug design and synthesis of
novel anti-malaria agents (supervisor prof. Ulrike Holzgrabe)
Projects
•
Title: Novel inhibitors of acetylcholinesterase derived from 7-MEOTA - potential
Alzheimer´s disease drugs (applicant prof. Kamil Kuca, co-applicant Dr. Daniela Ripova) –
Grant Agency of Czech Republic, 2011-2015, team-member)
•
PUBLICATIONS, CONFERENCES AND ORAL PRESENTATIONS
Conferences
1. Korabecny, J.; Kuca, K.; Musilek, K.; Opletalova, V.; Karasova, J.; Pohanka, M.
Synthesis and evaluation of bis-7-MEOTA compounds as reversible
acetylcholinesterase inhibitors. 9th International Conference Alzheimer’s and
Parkinson’s Diseases Prague (Czech Republic) 11.-15.3.2009, Neurodegenerative
Diseases 2009, 6 (S1), p. 2109, ISBN 978-3-8055-9118-8.
2. Pohanka, M.; Musilek, K.; Zdarova-Karasova, J.; Korabecny, J.; Drtinova, L.; Kassa,
J.; Kuca, K. In vitro evaluation of two Alzheimer’s disease drugs tacrine and 7methoxytacrine
using
electrochemical
biosensor
with
immobilized
acetylcholinesterase. 9th International Conference Alzheimer’s and Parkinson’s
Diseases Prague (Czech Republic) 11.-15.3.2009, Neurodegenerative Diseases 2009, 6
(S1), p. 2149, ISBN 978-3-8055-9118-8.
3. Stodulka, P.; Pohanka, M.; Musilek, K.; Korabecny, J.; Kuca, K.; Zdarova--Karasova,
J. In vitro study of passive drug transport through blood-brain barrier using HPLC
techniques. 9th International Conference Alzheimer’s and Parkinson’s Diseases
Prague (Czech Republic) 11.-15.3.2009, Neurodegenerative Diseases 2009, 6 (S1), p.
2112, ISBN 978-3-8055-9118-8.
4. Binder, J.; Holas, O.; Opletalova, V.; Kuca, K.; Musilek, K.; Korabecny, J.; Jun, D.
Design, synthesis and biological evaluation of new effective acetylcholinesterase
inhibitors. 10th International Meeting on Cholinesterases Sibenik (Croatia) 20.25.9.2009, Book of abstracts, P3-5, p. 92.
5. Korabecny, J.; Holas, O.; Opletalova, V.; Kuca, K.; Musilek, K.; Zdarova-Karasova,
J.; Synthesis amd evaluation of various N-methyl quarternary salts of 7methoxytacrine compounds as acetylcholinesterase inhibitors. 10th International 21,
p. 100.
6. Pohanka; M.; Drobik; Krenkova; Zdarova-Karasova, J.; Holas, O.; Kasalova;
Korabecny, J.; Marek, J.; Kuca, K.; Musilek, K. Electrochemical evaluation of
acetylcholinesterase activity and construction of biosensor suitable for anticholinergic
compounds assay. The 104th National Meeting of the Korean Chemical Society
Daejeon (Korea) 28.-30.10.2009, Abstract book p 255.
7. Binder, J.; Kuca, K.; Jun, D.; Korabecny, J.; Opletalova V. Design, syntéza a
biologické testování nových inhibitorů acetylcholinesterasy. 38. konference Syntéza a
analýza léčiv Hradec Králové (Česká republika) 14.-16.9.2009, Sborník p. 68.
8. Korabecny, J.; Holas, O.; Opletalova, V.; Musilek, K.; Kuca, K. Syntéza a in vitro
stanovení sekundárních alkyl-aminoderivátů odvozených od 7-MEOTA. 38.
konference Syntéza a analýza léčiv Hradec Králové (Česká republika) 14.-16.9.2009,
Sborník p. 102.
9. Korabecny, J.; Holas, O.; Musilek, K.; Opletalova, V.; Binder, J.; Pohanka, M.;
Zdarova-Karasova J.; Kuca, K. Syntéza a in vitro evaluace centrálně účinných
inhibitorů acetylcholinesterázy odvozených od struktury 7-MEOTA. 9. konference
odborné Společnosti vojenských lékařů, farmaceutů a veterinárních lékařů ČLS JEP
Hradec Králové (Česká republika) 26.-27.11.2009, Sborník příspěvků, p. 80-83.
10. Korabecny, J.; Holas, O.; Musilek, K.; Opletalova, V.; Pohanka, M.; Kuca, K. Nově
připravené deriváty látky 7-MEOTA. 52. Česko-Slovenská psychofarmakologická
konference Lázně Jeseník (Česká republika) 6.-10.1.2010, Supplementum 1, 2010, p.
45.
11. Korabecny, J.; Holas, O.; Patocka, J.; Zdarova-Karasova J.; Pohanka, M.; Opletalova,
V.; Musilek, K.; Kuca, K. Syntéza a in vitro testování strukturně odlišných alkylaminoderivátů odvozených od látky 7-MEOTA. 52. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 6.-10.1.2010,
Supplementum 1, 2010, p. 45.
12. Zdarova-Karasova, J.; Komloova, M.; Korabecny, J.; Musilek, K.; Kuca, K.
Hodnocení schopnosti prostupu léčiv, inhibitorů acetylcholinesterázy, přes
hematoencefalickou bariéru pomocí in vitro metodiky. 52. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 6. -10. 1. 2010,
Supplementum 1, 2010, p. 47.
13. Korabecny, J.; Holas, O.; Binder, J.; Zemek, F.; Marek, J.; Musilek, K.; Pohanka, M.;
Opletalova, V.; Dohnal, V.; Kuca, K. Syntéza a in vitro hodnocení duálních inhibitorů
cholinesteras se strukturním základem 7-MEOTA. 39. konference Syntéza a analýza
liečiv Modra-Harmónia (Slovenská republika) 2. -4. 9. 2010 zborník, p. 84.
14. Korabecny, J.; Holas, O.; Zemek, F.; Marek, J.; Musilek, K.; Pohanka, M.; Opletalova,
V.; Dohnal, V.; Kuca, K. Syntéza a hodnocení biologické účinnosti nových
takrinových derivátů jako potenciálních agens pro Alzheimerovu chorobu. 53. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 5. -9. 1.
2010, Supplementum 1, 2011, p. 55
15. Kuca, K.; Korabecny, J.; Holas, O.; Zemek, F.; Musilek, K.; Pohanka, M.; Opletalova,
V.; Dohnal, V. Syntéza a in vitro hodnocení N-alkyl-7-methoxytakrin hydrochloridů
jako potenciálních inhibitorů cholinesteras při Alzheimerově chorobě. 53. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 5. -9. 1.
2010, Supplementum 1, 2011, p. 56
16. Hroudova, J.; Fisar, Z.; Korabecny, J.; Kuca, K. In vitro účinky takrinu, 7-MEOTA a
oximů na aktivitu MAO-A, MAO-B a komplexu I dýchacího řetězce. 53. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 5. -9. 1.
2010, Supplementum 1, 2011, p. 55
17. Musilek, K.; Korabecny, J.; Holas, O.; Horova, A.; Patocka, J.; Kuca, K. 7-MEOTA –
cholinesterase inhibitor with valuable pharmacological profile. 10th International
Conference Alzheimer’s and Parkinson’s Diseases Barcelona (Spain) 9. -13.3.2011, p.
73.
18. Korabecny, J.; Musilek, K.; Holas, O.; Pohanka, M.; Opletalova, V.; Dohnal, V.;
Hroudova, J.; Jun, D.; Fisar, Z.; Karasova, J.; Patocka, J.; Kuca, K. Synthesis and in
vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential antiAlzheimer`s disease agents. 10th International Conference Alzheimer’s and
Parkinson’s Diseases Barcelona (Spain) 9. -13.3.2011, p. 74.
19. Pohanka, M.; Novotny, L.; Sobotka, J.; Korabecny, J.; Kuca, K. Metrifonate
(trichlorfon), an inhibitor of acetylcholinesterase is implicited in cerebral cortex
oxidative stress modulation. 10th International Conference Alzheimer’s and
Parkinson’s Diseases Barcelona (Spain) 9. -13.3.2011, p. 72.
20. Korabecny, J.; Musilek, K.; Holas, O.; Opletalova, V.; Dohnal, V.; Hroudova, J.;
Fisar, Z.; Patocka, J.; Kuca, K. 7-MEOTA derivatives based human cholinesterase
inhibitors. 12th Annual Network Conference Alzheimer’s Research UK Leeds (United
Kingdom) 16. – 17. 3. 2011, p. 36.
21. Musilek, K.; Korabecny, J.; Holas, O.; Horova, A.; Patocka, J.; Kuca, K. 7-MEOTA –
cholinesterase inhibitor with improved pharmacological properties. 12th Annual
Network Conference Alzheimer’s Research UK Leeds (United Kingdom) 16. – 17. 3.
2011, p. 46.
22. Korabecny, J.; Marek, J.; Musilek, K.; Kuca, K. Development of new 7-MEOTA
compounds: molecular modelling, synthesis and in vitro data. Twelfth Tetrahedron
Symposium Sitges (Spain) 21. -24. 6. 2011.
23. Korabecny, J.; Janovec, L.; Musilek, K.; Zemek, F.; Horova, A.; Nepovimova, E.;
Opletalova, V.; Hroudova, J.; Fisar, Z.; Jung, Y.-S.; Kuca, K. Comparison of novel
tacrine and 7-MEOTA derivatives with aromatic and alicyclic residues: synthesis,
biological evaluation and docking studies. 63. Zjazd Chemikov Vysoké Tatry,
Tatranské Matliare (Slovenská republika) 5. – 9. 9. 2011, Erratum.
24. Kuca, K.; Musilek, K.; Jun, D.; Pohanka, M.; Zdarova-Karasova, J.; Soukup, O.;
Marek, J.; Korabecny, J.; Hrabinova, M.; Kassa, J. Vývoj nových reaktivátorů
acetylcholinesterázy – antidot pro případ otrav organofosforovými pesticidy. 63. Zjazd
Chemikov Vysoké Tatry, Tatranské Matliare (Slovenská republika) 5. – 9. 9. 2011, p
225.
25. Marek, J.; Korabecny, J.; Musilek, K.; Cabal, J.; Kuca, K. Development of novel
quaternary detergents as part of decontamination and disinfection means. 63. Zjazd
Chemikov Vysoké Tatry, Tatranské Matliare (Slovenská republika) 5. – 9. 9. 2011, p
228.
26. Hroudova, J.; Fisar, Z.; Jirak, R.; Korabecny, J.; Kuca, K.; Raboch, J. Changes of
cellular respiration in patients with Alzheimer’s disease. 20. Evropský psychiatrický
kongres Praha (Česká republika) 3. 3. – 6. 3. 2012.
27. Korabecny, J.; Janovec, L.; Musilek, K.; Zemek, F.; Horova, A.; Nepovimova, E.;
Opletalova, V.; Hroudova, J.; Fisar, Z.; Jung, Y.-S.; Kuca, K. Comparison of novel
tacrine and 7-MEOTA derivatives with aromatic and alicyclic residues: synthesis,
biological evaluation and docking studies. 11. Conference Odborné společnosti
vojenských lékařů, farmaceutů a veterinárních lékařů ČLS Hradec Králové (Česká
republika) 18. – 19. 10. 2011, Blok V : Postery.
28. Hroudova, J.; Fisar, Z.; Jirak, R.; Korabecny, J.; Raboch, J. Změny bunečného dýchání
u pacientů s Alzheimerovou chorobou a osob v depresivní episodě. 54. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 4. -8. 1.
2012.
29. Korabecny, J.; Musilek, K.; Zemek, F.; Horova, A.; Holas, O.; Nepovimova, E.;
Opletalova, V.; Hroudova, J.; Fisar, Z.; Jung, Y.-S.; Kuca, K. Synthesis and in vitro
evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine – new
tacrine
derivative
with
cholinergic
properties.
54.
Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 4. -8. 1. 2012.
30. Korabecny, J.; Musilek, K.; Zemek, F.; Horova, A.; Nepovimova, A.; Opletalova, V.;
Hroudova, J.; Fisar, Z.; Jung, Y.-S.; Kuca, K. Monosubstitued N-alkylated-tacrine
derivatives: synthesis, biological evaluation and molecular modeling. 54. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 4. -8. 1.
2012.
31. Spilovska, K.; Hamuľakova, S.; Korabecny, J.; Musilek, K.; Kuca, K.; Imrich, J.
Synthesis and biological evaluation of tacrine-coumarine heterodimers as potential
cholinesterase inhibitors in Alzheimer's disease therapy. 54. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 4. -8. 1. 2012.
32. Hroudova, J.; Fisar, Z.; Kitzlerova E., Zverova, M.; Korabecny, J.; Kuca, K., Raboch,
J. Changes of cellular respiration in patients with depression. World Psychiatric
Association International Congress 2012. Praha (Česká republika) 17. – 21. 10. 2012.
33. Musilek, K.; Benek, O.; Korabecny, J.; Kuca, K.; Gunn-More, F. Analogues of
benzothiazole ureas as potential inhibitors of mitochondrial enzymes with implications
for AD. Alzheimer’s Research UK Conference 2012 Birmingham (United Kingdom)
27. – 28. 3. 2012, p. 64.
34. Korabecny, J.; Musilek, K.; Zemek, F.; Horova, A.; Holas, O.; Nepovimova, E.;
Opletalova, V.; Hroudova, J.; Fisar, Z.; Jung, Y.-S.; Kuca, K. Synthesis and in vitro
evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine – new
tacrine derivative with cholinergic properties. Alzheimer’s Research UK Conference
2012 Birmingham (United Kingdom) 27. – 28. 3. 2012, p. 46.
35. Korabecny, J.; Hamuľakova, S.; Babkova, K.; Horova, A.; Musilek, K.; Spilovska, K.;
Imrich, J.; Opletalova, V.; Gazova Z.; Karasova-Zdarova J.; Hroudova J.; Fisar Z.;
Gaľa L.; Valko M.; Kassa J.; Kuca K.; Synthesis, biological assessment and
molecular modeling of novel tacrine-7 methoxytacrine heterodimers for Alzheimer
disease treatment. 12th International Stockholm/Springfield Symposium on Advances
in Alzheimer Therapy Stockholm (Sweden) 9. – 12. 5. 2012, p. 80E.
36. Ricny, J.; Kristofikova Z.; Korabecny, J.; Kuca, K.; Musilek, K.; Proska, J.; Ripova,
D. Methoxytacrine analogues (N-alkyl-7-methoxytacrine hydrochlorides) as
acetylcholinesterase inhibitors with potential therapeutic use in Alzheimer disease.
12th International Stockholm/Springfield Symposium on Advances in Alzheimer
Therapy Stockholm (Sweden) 9. – 12. 5. 2012, p. 120E.
37. Drtinova, L.; Pohanka, M.; Sepsova, V.; Zemek, F.; Zdarova-Karasova, J.; Krenkova,
Z.; Misik, J.; Korabecny, J. HI-6 and obidoxime implication in oxidative stress: guinea
pig model. 11th international Meeting on Cholinesterases Kazan (Russia) 4. – 9. 6.
2012, p 2-9.
38. Korabecny, J.; Hamuľakova, S.; Babkova, K.; Horova, A.; Musilek, K.; Spilovska, K.;
Imrich, J.; Opletalova, V.; Gazova Z.; Karasova-Zdarova J.; Hroudova J.; Fisar Z.;
Gaľa L.; Valko M.; Kassa J.; Kuca K.; Synthesis, biological assessment and
molecular modeling of novel tacrine-7 methoxytacrine heterodimers for Alzheimer
disease treatment. 11th international Meeting on Cholinesterases Kazan (Russia) 4. –
9. 6. 2012, p 2-14.
39. Korabecny, J.; Nepovimova, E.; Janovec, L.; Horova, A.; Zemek, F.; Musilek, K.;
Spilovska, K.; Opletalova, V.; Kuca, K. Novel and re-evaluated activities in the series
of N-alkylated-tacrine derivatives: Synthesis, biological evaluation and molecular
modelling. 11th international Meeting on Cholinesterases Kazan (Russia) 4. – 9. 6.
2012, p 2-19.
40. Sepsova, V.; Krusek, J.; Soukup, O.; Zemek, F.; Drtinova, L.; Korabecny, J.;
Krenkova, Z.; Zdarova-Karasova, J. The interaction of reversible acetylcholinesterase
inhibitors with the nicotinic receptors – in vitro testing. 11th international Meeting on
Cholinesterases Kazan (Russia) 4. – 9. 6. 2012, p 7-10.
41. Hroudová J., Fišar Z., Kitzlerová E., Zvěřová M., Korábečný J., Kuča K., Raboch J.
Changes of cellular respiration in patients with depression. WPA International
Congress 2012, 17. – 21. 10. 2012 Prague (Czech Republic). Čes a slov Psychiat
2012; 108 (Suppl 1): 246. ISSN 1212-0383.
42. Zemek, F.; Sepsova, V.; Drtinova, L.; Korabecny, J.; Pohanka, M.; Zdarova-Karasova,
J.; Kuca, K. Interaction of acetylcholinesterase reactivators with albumin. P.8.b. Other
topcis (basic), P.8.b.001; Eur. Neuropsychopharm. S439-S440. (IF2011 = 4.046) 25th
ECNP Congress, 13-17 October 2012, Vienna, Austria
43. Zdarova-Karasova, J.; Hroch, M.; Korabecny, J.; Zemek, F.; Hrabinova, M.; Sepsova,
V.; Kuca, K. Takrin a jeho deriváty 7-MEOTA a KB-38: Hodnocení základních
farmakokinetických parametrů po i.m. podání u potkana. 55. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 4.-8.1.2013,
Supplementum 1, 2013, p. 65.
44. Hroudova, J.; Fisar, Z.; Raboch, J.; Korabecny, J.; Kuca, K. In vitro účinky inhibitorů
acetylcholinesteráz na aktivitu monoaminooxidáz a NADH dehydrogenázy. 55.
Česko-Slovenská psychofarmakologická konference Lázně Jeseník (Česká republika)
4.-8.1.2013, Supplementum 1, 2013, p. 65.
45. Spilovska, K.; Korabecny, J.; Musilek, K.; Horova, A.; benek, O.; Kuca, K. Synthesis
and biological testing of 7-methoxytacrine-adamantylamine heterodimers as potential
cholinesterase inhibitors in
Alzheimer disease. 55. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 4.-8.1.2013,
Supplementum 1, 2013, p. 66.
46. Sepsova, V.; Soukup, O.; Drtinova, L.; Korabecny, J.; Spilovska, K.; ZdarovaKarasova, J. Vliv inhibitorů acetylcholinesterasy na cholinergní system. 55. ČeskoSlovenská psychofarmakologická konference Lázně Jeseník (Česká republika) 4.8.1.2013, Supplementum 1, 2013, p. 66.
47. Korabecny, J.; Babkova, K.; Hamulakova, S.; Cabelova, P.; Nepovimova, E.; Andrs,
M.; Spilovska, K.; Benek, O.; Musilek, K.; Opletalova, V.; Hroudova, J.; Fisar, Z.;
Kuca, K. Synthesis, biological assessment and molecular modeling of novel tacrine-7methoxytacrine heterodimers for Alzheimer disease treatment. 55. Česko-Slovenská
psychofarmakologická konference Lázně Jeseník (Česká republika) 4.-8.1.2013,
Supplementum 1, 2013, p. 67.
48. Cabelova, P.; Korabecny, J.; Babkova, K.; Nepovimova, E.; Andrs, M.; Spilovska, K.;
Benek, O.; Musilek, K.; Opletalova, V.; Hroduova, J.; Fisar, Z.; Kuca, K. Synthesis,
biological properties and in silico studies in the series of novel 7-methoxytacrinedonepezil-like compounds. 55. Česko-Slovenská psychofarmakologická konference
Lázně Jeseník (Česká republika) 4.-8.1.2013, Supplementum 1, 2013, p. 67.
49. Marek, J.; Korabecny, J.; Babkova, K.; Hamulakova, S.; Cabelova, P.; Nepovimova,
E.; Andrs, M.; Spilovska, K.; Benek, O.; Musilek, K.; Opletalova, V.; Hroudova, J.;
Fisar, Z.; Kuca, K. Comparative study in the N-alkylated desries of tacrine and 7methoxytacrine derivatives. 55. Česko-Slovenská psychofarmakologická konference
Lázně Jeseník (Česká republika) 4.-8.1.2013, Supplementum 1, 2013, p. 68.
50. Korabecny, J.; Babkova, K.; Hamulakova, S.; Cabelova, P.; Nepovimova, E.; Andrs,
M.; Spilovska, K.; Benek, O.; Musilek, K.; Opletalova, V.; Hroudova, J.; Fisar, Z.;
Kuca, K. 7-methoxytacrine analogues as candidates for Alzheimer disease treatment.
55. Česko-Slovenská psychofarmakologická konference Lázně Jeseník (Česká
republika) 4.-8.1.2013, Supplementum 1, 2013, p. 68.
51. Benek, O.; Musilek, K.; Kuca, K.; Korabecny, J.; Spilovska, K.; Gunn-Moore, F.
Benzothiazolyl urea analogues as inhibitors of ABAD-Aβ interaction in Alzheimer
disease. 55. Česko-Slovenská psychofarmakologická konference Lázně Jeseník (Česká
republika) 4.-8.1.2013, Supplementum 1, 2013, p. 68.
52. Korabecny, J.; Cabelova, P.; Babkova, K.; nepovimova, E.; Andrs, M.; Spilovska, K.;
Benek, O.; Musilek, K.; Opletalova, V.; Hroudova, J.; Fisar, Z.; Kuca, K. Synthesis,
biological properties and in silico studies in the series of novel 7-methoxytacrinedonepezil like compounds. 11th International Conference On Alzheimer’s and
Parkinson’s Diseases Florence (Italy) 6. -10. 3. 2013
53. Soukup, O.; Korabecny, J.; Musilek, K.; Jun, D.; Misik, J.; Zdarova-Karasova, J.;
Kamil, K. Hybrids of AChE inhibitor and memantine derivatives as candidates for
Alzheimer’s disease treatment. Neuroscience 2013 San Diego (California, USA) 9. –
13. 11. 2013.
54. Kuca, K.; Musilek, K.; Jun, D.; Zdarova-Karasova, J.; Kunes, M.; Soukup, O.;
Korabecny, O.; Sepsova, V.; Hrabinova, M. Novel acetylcholinesterase reactivators –
antidotes against nerve agents. International Conference on Pharmacology and Drug
Development Singapore (Singapore) 9. – 11. 12. 2013.
55. Korabecny, J.; Cabelova, P.; Nepovimova, E.; Andrs, M.; Spilovska, K.; Musilek, K.;
Opletalova, V.; Kuca, K. 7-MEOTA-DONEPEZIL-LIKE COMPOUNDS FOR
ALZHEIMER’S DISEASE TREATMENT. XXIII International Symposium on
Medicinal Chemistry Lisbon (Portugal) 7.-11.9.2014.
56. Andrs, M.; Korabecny, J.; Babkova, K.; Musilek, K.; Kuca, K. Synthesis, biological
assessment and molecular modelling of tacrine-7-methoxytacrine heterodimers for
Alzheimer’s disease treatment. TOXCON, Stará Lesná, Vysoké Tatry (Slovakia) 24.26.11.2014.
57. Drtinova, L.; Pohanka, M.; Spilovska, K.; Korabecny, J.; Sepsova, V.; Nepovimova,
E.; Kuca, K. New cholinestearse inhibitors 7-methoxytacrine-adamantylamine
heterodimers as inhibitors of BACE and amyloid beta 1-40. TOXCON, Stará Lesná,
Vysoké Tatry (Slovakia) 24.-26.11.2014.
58. Misik, J.; Korabecny, J.; Nepovimova, E.; Kassa, J. Therapeutic effect of novel Nalkylated tacrine analogues on cognitive deficit induced by 3-quinicidinyl benzilate in
rats performing the water maze. TOXCON, Stará Lesná, Vysoké Tatry (Slovakia) 24.26.11.2014.
59. Nepovimova, E.; Korabecny, J.; Dolezal, R.; Cabelova, P.; Musilek, K.; Kuca, K. 7
MEOTA-donepezil like compounds – novel agents to combat Alzheimer’s disease.
TOXCON, Stará Lesná, Vysoké Tatry (Slovakia) 24.-26.11.2014.
60. Korabecny, J.; Nepovimova, E.; Soukup, O.; Sepsova, V.; Bolognesi, M.L.; Kuca, K.;
Bartolini, M. Multitarget drug design strategy: quinone-tacrine hybrids designed to
block amyloid-beta aggregation and to exert anticholinesterase and antioxidant effects.
NEURODEGENERATIVE DISEASES: BIOLOGY & THERAPEUTICS, Cold
Spring Harbor, New York (USA) 3.-6.12.2014.
61. Patocka, J.; Korabecny, J.; Soukup, O.; Sepsova, V.; Nepovimova, E.; Jun, D.; Kuca,
K. Possible role of hydroxylated metabolites of tacrine in drug toxicity and therapy of
Alzheimer's disease. NEURODEGENERATIVE DISEASES: BIOLOGY &
THERAPEUTICS, Cold Spring Harbor, New York (USA) 3.-6.12.2014.
62. Nepovimova, E.; Korabecny, J.; Cabelova, P.; Soukup, O.; Sepsova, V.; Kuca, K. 7MEOTA-donepezil like compounds – novel agents to combat Alzheimer’s disease.
NEURODEGENERATIVE DISEASES: BIOLOGY & THERAPEUTICS, Cold
Spring Harbor, New York (USA) 3.-6.12.2014.
63. Sepsova, V.; Nepovimova, E.; Korabecny, J.; Krusek, J.; Tobin, G.; Zdarova, J.; Kuca,
K.; Soukup. O.; New 7-MEOTA-donepezil derivatives modulate acetylcholinesterase
and cholinergic receptors. NEURODEGENERATIVE DISEASES: BIOLOGY &
THERAPEUTICS, Cold Spring Harbor, New York (USA) 3.-6.12.2014.
64. Soukup. O.; Sepsova, V.; Korabecny, J; Nepovimova, E.; Kuca, K. A resurrection of
7-MEOTA? A comparison with tacrine. NEURODEGENERATIVE DISEASES:
BIOLOGY & THERAPEUTICS, Cold Spring Harbor, New York (USA) 3.6.12.2014.
65. Nepovimova, E.; Korabecny, J.; Bartolini, M.; Bergamini, C.; Lamba, D.; Roberti, M.;
Monti, B.; Kuca, K.; Bolognesi, M.L. Multitarget drug design strategy: Quinonetacrine hybrids designed to block amyloid-beta aggregation and to exert
anticholinesterase and antioxidant effects. 12th International Conference on
Alzheimer's and Parkinson's Diseases and Related Neurological Disorders (AD/PDTM
2015), Nice, France, 18-22.3.2015.
66. Korabecny, J.; Cabelova, P.; Dolezal, R.; Nepovimova, E.; Babkova, K.; Spilovska,
K.; Andrs, M.; Musilek, K.; Soukup, O.; Kuca, K. 7-MEOTA-donepezil like
compounds – novel agents to combat Alzheimer’s disease. 12th International
Conference on Alzheimer's and Parkinson's Diseases and Related Neurological
Disorders (AD/PDTM 2015), Nice, France, 18-22.3.2015.
67. Korabecny, J.; Cabelova, P.; Dolezal, R.; Nepovimova, E.; Babkova, K.; Spilovska,
K.; Andrs, M.; Musilek, K.; Soukup, O.; Kuca, K. 7-MEOTA-donepezil like
compounds – novel agents to combat Alzheimer’s disease. 12th International Meeting
on Cholinesterases-Sixth International Conference on Paraoxonases, Alicante, Spain,
27.9.-2.10.2015.
Oral presentations
1. Korabecny, J. Nové deriváty 7-methoxytakrinu jako potenciální léčiva Alzheimerovy
choroby; 26. 10. 2011, Košice.
2. Korabecny, J. Syntéza, biologické hodnocení a molekulární docking nových takrin-7methoxytakrin heterodimerů pro léčbu Alzheimerovy choroby; Studentská vědecká
konference, 1. 2. 2012, Hradec Králové.
3. Korabecny, J.; Hamulakova, S.; Kuca, K.; Musilek, K.; Kassa, J. Syntéza, biologické
vlastnosti a molekulově modelovací studie takrin-7-methoxytakrin heterodimerů v
terapii Alzheimerovy choroby; Květinův den 2012, 31. 5. 2012, Brno.
4. Korabecny, J.; Hamulakova, S.; Babkova, K.; Horova, A.; Musilek, K.; Spilovska, K.;
Imrich, J.; Opletalova, V.; Gazova, Z.; Hroudova, J.; Fisar, Z.; Gala, L.; Valko, M.;
Kassa, J.; Kuca, K. Synthesis, biological assessment and molecular modelling of
tacrine-7-methoxytacrine heterodimers for Alzheimer disease treatment. 2nd Meeting
of the Paul Ehrlich MedChem Euro-PhD Network 2012, O-37, 9. 9. -11. 9. 2012
Ljubljana, Slovenia.
5. Korabecny, J. Design and synthesis of uncharged reactivators against
organophosphorus nerve agents poisoned cholinesterases. Institut Francais de Prague,
7. 4. 2013, Prague, Czech Republic.
6. Korabecny, J.; Nepovimova, E.; Spilovska, K.; Andrs, M.; Babkova, K.; Musilek, K.;
Kassa, J.; Kuca, K. Development of tacrine derivatives for Alzheimer’s disease at the
department of toxicology in Hradec Kralove. TOXCON, Interdisciplinary Toxicology.
2014; Vol. 7(Suppl. 1), 7, 24.-26.9.2014, Stará Lesná, Vysoké Tatry, Slovakia.
7. Korabecny, J. Drug development for Alzheimer’s disease in Hradec Kralove.
Workshop on Italy-Czech cooperation on AD and other related topics., 28.-30.9.2014,
Bologna, Italy.
8. Korabecny, J. Development of Novel Multi-Target Directed Ligands for Alzheimer’s
Disease. Biomedical Research Center group meeting, Rusalka, Malá Úpa, 15.17.1.2015, Czech Republic.
9. Korabecny, J.; Nepovimova, E.; Spilovska, K.; Andrs, M.; Babkova, K.; Musilek, K.;
Soukup, O.; Kuca, K. Drug Design and Development of Novel Drugs for Alzheimer’s
Disease Treatment. 5th PhD and 3rd Postdoc Conference FaF UK, 3.-4.2.2015, Hradec
Králové, Czech Republic.
10. Kuca, K.; Novotny,M.; Uhrikova, A.; Sevimli, A.; Soukup, O.; Rousar, T.; Jost, P.;
Jun, D.; Korabecny, J.; Musilek, K. Modified bisquaternary monooximes were found
to be effective reactivators of human AChE inhibited by organophosphates. 1st
International Scientific Conference, CBRN, Research & Innovation, 16.-18.3.2015,
Antibes - Juan-les-Pins, France.
11. Kuca, K.; Hamulakova, S.; Janovec, L.; Hrabinova, M.; Spilovska, K.; Korabecny, J.;
Kristian, P.; Nepovimova, E.; Maresova, P.; Imrich, J. Synthesis and biological
evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase
inhibitors. Drug Discovery and Therapy World Congress 2015, 22.-25.7.2015, Boston,
MA, USA
Book chapters
1. Korabecny, J.; Zemek, F.; Soukup, O.; Spilovska, K.; Musilek, K.; Jun, D.;
Nepovimova, E.; Kuca, K. Current treatment and perspectives in pharmacotherapy of
Alzheimer`s disease. Frontiers in Drug Discovery, 2014, 6, 702 738.
2. Musilek, K.; Korabecny, J.; Jun, D.; Kassa, J.; Kuca, K. Novel cholinesterase
inhibitors. Handbook of Toxicology of Chemical Warfare Agents. 2015, 1071 1087.
Published papers
1. Pohanka, M.; Zdarova Karasova, J.; Kuca, K.; Pikula, J.; Holas, O.; Korabecny, J.;
Cabal, J. Colorimetric dipstick for assay of organophosphate pesticides and nerve
agents represented by paraoxon, sarin and VX. Talanta. 2010, 81, 621 624. IF = 3.722
2. Korabecny, J.; Musilek, K.; Holas, O.; Binder, J.; Zemek, F.; Marek, J.; Pohanka, M.;
Opletalova, V.; Dohnal, V.; Kuca, K. Synthesis and in vitro evaluation of N alkyl-7methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer
disease. Bioorg. Med. Chem. Lett. 2010, 20, 6093 6095. IF = 2.661
3. Kuca, K.; Marek, J.; Zdarova Karasova, J.; Pohanka, M.; Korabecny, J.; Kalasz, H.
Novel Acetylcholinesterase reactivator – oxime K048 – reactivation activity in vitro.
Med. Chem. 2010, 1 5.
4. Korabecny, J.; Holas, O.; Musilek, K.; Pohanka, M.; Opletalova, V.; Dohnal, V.;
Kuca, K. Synthesis and in vitro evaluation of new tacrine derivates-bis- alkylene
linked 7-MEOTA. Lett. Org. Chem. 2010, 7, 327 331. IF = 0.774
5. Marek, J.; Stodulka, P.; Cabal, J.; Soukup, O.; Pohanka, M.; Korabecny, J.; Musilek,
K.; Kuca, K. Preparation of the pyridinium salts differing in the length of the N-alkyl
substituent. Molecules 2010, 15, 1967 1972.
6. Korabecny, J.; Musilek, K.; Holas, O.; Nepovimova, E.; Jun, D.; Zemek, F.;
Opletalova, V.; Patocka, J.; Dohnal, V.; Nachon, F.; Hroudova, J.; Fisar, Z.; Kuca, K.
Synthesis and in vitro evaluation of N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4tetrahydroacridin-9-amine as a cholinesterase inhibitor with regard to Alzheimer’s
dinase treatment. Molecules 2010, 15, 8804 8812. IF = 1.738
7. Fisar, Z.; Hroudova, J.; Korabecny, J.; Musilek, K.; Kuca, K. In vitro effects of
acetylcholinesterase reactivators on monoamine oxidase activity. Toxicol. Lett. 2011,
201, 176 180.
8. Jun, D.; Musilek, K.; Kassa, J.; Cabal, J.; Zdarova-Karasova, J.; Pohanka, M.; Bajgar,
J.; Marek, J.; Komloova, M.; Soukup, O.; Holas, O.; Korabecny, J.; Dolezal, B.; Kuca,
K. Vývoj univerzálního antidota otrav nervově paralytickými látkami na bázi
reaktivátorů cholinesteráz: Od substance k autoinjektoru. Urgentní medicína 2010, 4,
15 19.
9. Hroudova, J.; Fisar, Z.; Korabecny, J.; Kuca, K. In vitro effects of acetylcholinesterase
inhibitors and reactivators on Complex I of electron transport chain. Neuroendocrinol.
Lett. 2011; 32, 259 263.
10. Korabecny, J.; Musilek, K.; Horova, A.; Holas, O.; Nepovimova, E.; Opletalova, V.;
Hroudova, J.; Fisar, Z.; Jung, Y. S.; Kuca, K. Synthesis and in vitro evaluation of 7methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine - new tacrine derivate
with cholinergic properties. Bioorg. Med. Chem. Lett. 2011; 21, 6563 6566.
11. Korabecny, J.; Janovec, L.; Musilek, K.; Zemek, F.; Horova, A.; Nepovimova, E.;
Dolezal, R.; Opletalova, V.; Hroudova, J.; Fisar, Z.; Jung, Y. S.; Kuca, K. Comparison
of novel tacrine and 7-MEOTA derivatives with aromatic and alicyclic residues:
Synthesis, biological evaluation and docking studies. Lett. Org. Chem. 2013; 10, 291
297.
12. Zdarova-Karasova, J.; Korabecny. J.; Pohanka, M.; Zemek, F.; Sepsova, V.; Kuca, K.
Acetylcholinesterase inhibitors used or tested in Alzheimer Disease therapy; their
passive diffusion through blood brain barrier: In vitro study. Afr. J. Pharm. Pharmaco.
2013, 7, 1471-1481.
13. Korabecny, J.; Hruba, E.; Soukup. O.; Zemek, F.; Musilek, K.; Nepovimova, E.;
Spilovska, K.; Opletalova, V.; Kuca, K. Zvažovane farmakoterapeutické přístupy
léčby Alzheimerovy choroby. Česk. slov. Farm. 2012, 61, 4 10.
14. Soukup, O.; Jun, D.; Karasova-Zdarova, J.; Patocka, J.; Musilek, K.; Korabecny, J.;
Krusek, J.; Kaniakova, M.; Sepsova, V.; Mandikova, J.; Trejtnar, F.; Pohanka, M.;
Drtinova, L.; Pavlik, M.; Tobin, G.; Kuca, K. A resurrection of 7-MEOTA: a
comparison with tacrine. Curr. Alzheimer Res. 2013, 10, 893-906. IF = 3.796
15. Spilovska, K.; Korabecny, J.; Kuca, K.; Musilek, K. Inhibítory gamma sekretázy v
terapii Alzheimerovej choroby. Ceska Slov. Farm. 2012, 61, 93 100.
16. Zemek, F.; Korabecny, J.; Sepsova, V.; Karasova-Zdarova, J.; Musilek, K.; Kuca, K.
Albumin and Alpha 1-Acid Glycoprotein; An Old Acquaintance. Expert Opin. Drug
Metab. Toxicol. 2013, 9, 943-954.
17. Sepsova, V.; Zdarova-Karasova, J.; Korabecny, J.; Zemek, F.; Bennion, B.J.; Kuca, K.
Oximes: Inhibitors of human acetylcholinesterase – a structure-activity relationship
(SAR) study. Int. J. Mol. Sci. 2013, 14, 16882-16900.
18. Spilovska, K.; Korabecny, J.; Kral, J.; Horova, A.; Musilek, K.; Drtinova, L.; Gazova,
Z.; Siposova, K.; Kuca, K. 7-methoxytacrine-adamantylamine heterodimers as
cholinesterase inhibitors in AD treatment – synthesis, biological evaluation and
molecular modeling studies. Molecules, 2013, 18, 2397-2418. IF = 2.428
19. Korabecny, J.; Spilovska, K.; Benek, O.; Musilek, K.; Soukup, O.; Kuca, K. Takrin a
jeho deriváty v terapii Alzheimerovy choroby. Cesk. Slov. Farm. 2012, 61, 210-221.
20. Pohanka, M.; Cabal, J.; Bartosova, L.; Stetina, R.; Svobodova, H.; Zdarova-Karasova,
J.; Kracmarova, A.; Drtinova, L.; Pavlik, M.; Korabecny, J.; Sespova, V.; Kassa, J.
Vybrané laboratorní postupy v toxikologii. Studijní texty FVZ UO v Hradci Králové.
2012.
21. Zemek, F.; Sepsova, V.; Drtinova, L.; Nepovimova, E., Korabecny, J.; Kuca, K.
Outcomes of Alzheimer diseases therapy with acetylcholinesterase inhibitors and
memantine. Expert Opin. Drug Saf. 2014, 13, 759 774. IF = 2.735
22. Korabecny, J.; Soukup, O.; Dolezal, R.; Spilovka, K.; Nepovimova, E.; Andrs, M.;
Nguyen, T.D.; Jun, D.; Musilek, K.; Kucerova-Chlupacova, M.; Kuca, K. From
pyridinium-based to centrally active acetylcholinesterase reactivators. Mini-Rev. Med.
Chem. 2014, 14, 215 221. IF = 3.186
23. Valis, M.; Koci, J.; Tucek, D.; Lutonsky, O.; Kopova, J.; Barton, P.; Vysata, O.;
Krajickova, D.; Korabecny, J.; Masopust, J.; Klzo, L. Common yew intoxication: a
case report. Journal of Medical Case Reports. 2014, 8, 4.
24. Kassa, J.; Korabecny, J.; Sepsova, V.; Tumova, M. The evaluation of prophylactic
efficacy of newly developed reversible inhibitors of acetylcholinesterase in somanpoisoned mice – a comparison with commonly used pyridostigmine. Bas. Clin.
Pharmacol. Toxicol. 2014, 115, 571-576. IF = 2.294
25. Korabecny, J.; Dolezal, R.; Cabelova, P.; Horova, A.; Hruba, E.; Ricny, J.; Sedlacek,
L.; Nepovimova, E.; Spilovska, K.; Andrs, M.; Musilek, K.; Opletalova, V.; Sepsova,
V.; Ripova, D.; Kuca, K. 7-MEOTA-donepezil like compounds as cholinesterase
inhibitors: Synthesis, pharmacological evaluation, molecular modelling and QSAR
studies. Eur. J. Med. Chem. 2014, 82, 426 438. IF = 3.447
26. Spilovska, K.; Korabecny, J.; Horova, A.; Musilek, K.; Nepovimova, E.; Drtinova, L.;
Gazova, Z.; Siposova, K.; Dolezal, R.; Kuca, K. Design, synthesis and in vitro testing
of 7-methoxytacrine-amantadine analogues: A novel cholinesterase inhibitors for the
treatment of Alzheimer’s disease. Med. Chem. Res. 2015, 24, 2645-2655. IF = 1.402.
27. Nepovimova, E.; Korabecny, J.; Horova, A.; Musilek, K.; Dolezal, R.; Jung, Y.-S.;
Kuca, K. N-alkylated tacrine analogues as potential drugs for Alzheimer’s disease.
Drug. Des. Devel. Ther. 2015, submitted.
28. Sepsova, V.; Zdarova-Karasova, J.; Tobin, G.; Jun, D.; Korabecny, J.; Cabelova, P.;
Janska, K.; Krusek, J.; Kuca, K.; Soukup, O. Cholinergic properties of new 7
methoxytacrine-donepezil derivatives. Gen. Physiol. Biophys. 2015, 34, 189 200. IF=
0.875.
29. Andrs, M.; Korabecny, J.; Jun, D.; Hodny, Z.; Bartek, J.; Kuca, K.
Phosphatidylinositol 3-kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase
(PIKK) inhibitors: the importance of the morpholine ring. J. Med. Chem. 2015, 58, 41
71. IF = 5.480.
30. Andrs, M.; Korabecny, J.; Jun, D.; Kuca, K. The development of ataxia telangiectasia
mutated kinase inhibitors. Mini-Rev. Med. Chem. 2014, 14, 805 811. IF = 3.186
31. Dolezal, R.; Korabecny, J.; Honegr, J.; Malinak, D.; Musilek, K.; Kuca, K. Ligandbased 3D QSAR analysis of reactivation potency of mono- and bis- pyridinium
oximes toward VX-inhibited rat acetylcholinesterase. J. Mol. Graphics Model. 2015,
56, 113 129. IF = 2.022.
32. Korabecny, J.; Nepovimova, E.; Dolezal, R.; Malinak, D.; Soukup, O.; Andrs, M.;
babkova, K.; Sepsova, V.; Benek, O.; Hroch, L.; Kracmarova, A.; Hrabinova, M.;
Hrabcova, V.; Zemek, F.; Marek, J.; Honegr, J.; Jun, D.; Musilek, K.; Kuca, K.
Donepezil–from cholinesterase inhibitor to multi-target-directedligands. Prog.
Neurobiol., 2015, submitted.
33. Malinak, D.; Salajkova, S.; Dolezal, R.; Marek, J.; Soukup, O.; Vejsova, M.;
Korabecny, J.; Honegr, J.; Penhaker, M.; Musilek, K.; Kuca, K. Synthesis, biological
evaluation and LC-MS analysis of 6-hydroxyquinolinium salts differing in the length
of a side alkyl chain. Bioorg. Med. Chem. Lett. 2014, 24, 5238 5241. IF = 2.331
34. Hamulakova, S.; Janovec, L.; Hrabinova, M.; Spilovska, K.; Korabecny, J.; Kristian,
P.; Kuca, K.; Imrich, J. Synthesis and biological evaluation of novel tacrine
derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. J. Med. Chem.
2014, 57, 7073 7084. IF = 5.480.
35. Guest, P.; Benek, O.; Aitken, L.; Smith, T.K.; Korabecny, J.; Soukup, O.; Jun, D.;
Kuca, K.; Yan, S.S.; Gunn-Moore, F.; Musilek, K. The design, synthesis and
evaluation of benzothiazolylurea analogues as inhibitors of the amyloid binding
alcohol dehydrogenase / 17β-hydroxysteroid dehydrogenase type 10 enzyme. J. Med.
Chem. 2015 Submitted.
36. Nepovimova, E.; Uliassi, E.; Korabecny, J.; Peña-Altamira, L.E.; Samez, S.; Pesaresi,
A.; Garcia, G.E.; Bartolini, M.; Andrisano, V.; Bergamini, C.; Fato, R.; Lamba, D.;
Roberti, M. Kuca, K.; Monti, B.; Bolognesi, M.L. Multitarget drug design strategy:
quinone-tacrine hybrids designed to block amyloid-beta aggregation and to exert
anticholinesterase and antioxidant effects. J. Med. Chem. 2014, 57, 8576 8589. IF =
5.480.
37. Lee, S.K.; Park, M.K.; Yi, J.; Nahm, K.; Cho, D.W.; Ra, C.S.; Musilek, K.; Horova,
A.; Korabecny, J.; Dolezal, R.; Jun, D.; Kuca, K. Preparation of 7-methoxy tacrine
dimer analogues and their in vitro/in silico evaluation as potential cholinesterase
inhibitors. B. Korean Chem. Soc. 2015, 35(6), 1654-1660. IF = 0.835.
38. Andrs, M.; Korabecny, J.; Nepovimova, E.; Jun, D.; Hodny, Z.; Bartek, J.; Kuca, K.
Small molecules targeting ATR kinase: an emerging way to enhance existing cancer
therapy. Curr Cancer Drug target. 2015, just accepted. IF = 3.522.
39. Kuca, K.; Musilek, K.; Jun, D.; Soukup, O.; Korabecny, J. Oxime K074 – in vitro
reactivation of acetylcholinesterase inhibited by nerve agents and pesticides. J. Enzym.
Inhib. Med. Ch. 2015, submitted.
40. Misik, J.; Korabecny, J.; Nepovimova, E.; Cabelova, P.; Kassa, J. Effects of novel 7MEOTA-donepezil like hybrids and N alkylated tacrine analogues in the treatment of
quinuclidinyl benzilate-induced behavioural deficit in rats performing the multiple T
maze test. Biomed. Pap. Med. Fac. Univ. Palacky Olomouc Czech Repub. 2015, just
accepted. IF = 1.661.
41. Soukup, O.; Korabecny, J.; Honegr, J.; Kuca, K. Nové trendy ve vývoji nových léčiv
Alzheimerovy nemoci. Acta Medicinae, 2014, 11, 66-68.
42. Kuca, K.; Musilek, K.; Korabecny, J.; Zdarova-Karasova, J.; Soukup, O.; Hrabinova,
M.; Jun, D. Influence of the distance between quaternary nitrogen and oxime group on
the reactivation ability of oximes – antidotes against nerve agents. Journal of
Environmental Immunology and Toxicology, 2014, 1, 41-43
43. Malinak, D.; Gonda, J.; Korabecny, J.; Dolezal, R.; Honegr, J.; Soukup, O.; Buzga,
M.; Kuca, K. A review of total synthesis of (+) lactacystin and its analogs. Curr. Org.
Chem. 2015, 19 (20), 1980-2001. IF = 2.157.
44. Misik, J.; Korabecny, J.; Nepovimova, E.; Kracmarova, A.; Kassa, J. Effects of novel
tacrine-related cholinesterase inhibitors in the reversal of 3-quinuclidinyl benzilateinduced cognitive deficit in rats - is there a potential for Alzheimer's disease
treatment? Neurosci. Lett. 2015, submitted.
45. Nunes Lemes, L.F.; de Andrade Ramos, G.; de Oliveira, S.; R.da Silva, F.M.; de
Castro Couto, G.; da Silva Boni, M.; Guimarães, M.J.; O. Souza, I.N.; Bartolini, M.;
Andrisano, V.; do Nascimento Nogueira, P.C.; Rocha Silveira, E.; Soukup, O.;
Korabecny, J.; C. Romeiro, N.; G. Castro, N.; Bolognesi, M.L.; Soares Romeiro, L.A.
Cardanol-derived AChE inhibitors: towards the development of dual binding
derivatives for Alzheimer’s disease. Eur. J. Med. Chem. 2015, submitted.
46. Nepovimova, E.; Korabecny, J.; Dolezal, R. babkova, K.; Ondrejicek, A.; Jun, D.;
Sepsova, V.; Horova, A.; Hrabinova, M.; Soukup, O.; Bukum, N.; Jost, P; Muckova,
L.; Kassa, J.; Malinak, D.; Andrs, M.; Kuca, K. Tacrine – trolox hybrids: A novel
class of centrally active, non-hepatotoxic multi-target-directed ligands exerting
anticholinesterase and antioxidant activities with low in vivo toxicity. J. Med. Chem.
2015, submitted.
47. Prati, F.; Bergamini, C.; Fato, R.; Soukup, O.; Korabecny, J.; Andrisano, M.;
Bartolini, M.; Bolognesi, M.L. Novel 8-hydroxyquinoline derivatives as multitarget
compounds for the treatment of Alzheimer’s Disease. ChemMedChem., 2015,
submitted.
48. Spilovska, K.; Zemek, F.; Korabecny, J.; Nepovimova, E.; Soukup, O.; Windisch, M.;
Kuca, K. Adamantane – a lead structure for drugs in clinical practice. Expert Opin.
Drug Saf. 2015, submitted.
49. Andrs, M.; Muthna, D.; Rezacova, M.; Siman, P.; Korabecny, J.; Benek, O.; Dolezal,
R.; Soukup, O.; Jun, D.; Kuca, K. Novel caffeine derivatives with antiproliferative
activity. MedChemComm. 2015, submitted.
50. Kuca, K.; Soukup, O.; Maresova, P.; Korabecny, J.; Nepovimova, E.; Klimova, B.;
Honegr, J.; Ramalho, T.; Costa Franca, T. New trends in development of novel drugs
for Alzheimer’s disease. J. Braz. Chem. Soc. 2015, submitted.
51. Korabecny, J.; Andrs, M.; Nepovimova, E.; Dolezal, R.; Babkova, K.; Horova, A.;
Malinak, D.; Gorecki, L.; Mezeiova, E.; Sepsova, V.; Hrabinova, M.; Soukup, O.; Jun,
D.; Kuca, K. 7-Methoxytacrine-p-Anisidine Dimers as Novel Dual Binding Site
Acetylcholinesterase Inhibitors for Alzheimer's Disease Treatment. Molecules, 2015,
submitted.
52. Zdarova-Karasova, J.; Soukup, O.; Korabecny, J.; Hroch, M.; Sepsova, V.; Kuca, K.
Tacrine and its 7-methoxy derivate; significant differences in absorption and bloodbrain barrier penetration after oral application. J. Appl. Biomed. 2015, submitted.
53. Soukup, O.; Dolezal, R.; Malinak, M.; Marek, J.; Salajkova, S.; Pasdiorova, M.;
Honegr, J.; Korabecny, J.; Nachtigal, P.; Nachon, F.; Jun, D.; Kuca, K. Synthesis,
antimicrobial evaluation and molecular modeling of 5-hydroxyisoquinolinium salt
series; the effect of the hydroxyl moiety. Bioorg. Med. Chem. Lett. 2015, submitted.
Conference contributions
1. Dolezal, R.; Bodnarova, A.; Cimler, R.; Husakova, M.; Najman, L.; Racakova, V.;
Krenek, J.; Korabecny, J.; Kuca, K.; Krejcar, O. Variable elimination approaches for
data-noise reduction in 3D QSAR calculations. 17th Portuguese Conference on
Artificial Intelligence (EPIA-2015), 2015, 313-325, 8. -11. 9. 2015, Coimbra, Portugal
2. Balik, L.; Horalek, J.; Hornig, O.; Sobeslav, V.; Dolezal, R.; Korabecny, J.; Kuca, K.
Endpoint firewall for local security hardening in academic research environment.
ICCCI 2015 : 7th International Conference on Computational Collective Intelligence
Technologies and Applications. 21. – 23. 9. 2015, Madrid, Spain.