EVALUATION OF THE ACTIVITY NEW PIPERAZINEDIONE
DERIVATIVES
Nguyen Van A1, Tran Van B2
1
Insitute of Chemistry, Vietnam Academy of Scicence and Technology (VAST)
2
Vietnam National University, Hanoi (VNU)
1. SUMMARY
In this paper, several piperazinediones containing naphthalen moiety were
synthesized as (cyclo)tryprostatin analogues by Pictet-Spengler reaction through acylation
of the piperidine nitrogen, then condensation with primary amines such as n-propyl and nbutyl amine. These compounds were further treated with primary amines to afford the
corresponding diketopiperazines.
Keywords:
Pictet-Spengler,
(cyclo)tryprostatin
piperazinedione,
diketopiperazines,
activity,
2. INTRODUCTION
Piperazinediones are the class of truly ubiquitous structures involved in the
regulation of a wide variety of biological processes [1, 2]. The broad range of bioactivities
of these molecules has led to their description as ‘privileged structures’[3,4].
3. MATERIALS AND METHODS
3.1. Materials
3.2. Methods
4. RESULTS AND DISCUSSION
Fig. 1
Table 1. Cytotoxicity evaluation
1
IC50 (µg/mL)
Entry
compound
KB
Hep-G2
LU
MCF7
1
7a
62.31
>128
>128
>128
2
7b
>128
>128
>128
>128
3
8a
4.40
8.00
99.2
>128
4
8b
>128
>128
>128
>128
5
Ellipticine
0.625
0.625
0.625
0.625
Acknowledgements: This work was financially supported in part by scientific
research and technological development project (code: ĐT.NCCB-ĐHUD.2011-G/07)
5. CONCLUSIONS
6. REFERENCES
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1894.
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Schlitzer, M. Angew. (2004) Chem., Int. Ed., 43:251–254; (f) Horton, D. A.; Bourne, G. T. Smythe, M. L. (2003)
Chem. Rev. 103:893–930
3. Cui, C-B.; Kayeka, H.; Osada, H. (1996) J. Antiobiot., 49: 832-835.
2