Cytostatic and cytotoxic activity of synthetic diterpene derivatives obtained from (-)-Kaur-9(11),16-dien-19-oic acid against human cancer cell lines

被引：6

作者：

Alonso, R ^{[1
]}

Gomis, H

Taddei, A

Sajo, C

机构：

[1] Inst Venezolano Invest Cient, Ctr Quim, Caracas 1020A, Venezuela

[2] Univ Simon Bolivar, Dept Biol Celular, Caracas 1080A, Venezuela

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2005年 / 2卷 / 04期

关键词：

diterpene; kaurene; espeletia; antitumoral; cytostatic and cytotoxic;

D O I：

10.2174/1570180054038323

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

These diterpenes (1) and (2) were synthesized via epoxidation and rearrangements of (-)Kaur-9(11), 16-dien-19-oate (7) isolated from Venezuelan species of espeletia (frailejon), and their antimicrobial and antitumoral activity were evaluated. Compound (1) showed GI(50) values of 51.6 nM against CNS SF-539, LC50= 100 mu M, log(10) GI(50) = -7.29; compound (2) showed GI(50) at 4.17 mu M against breast cancer T47D, LC50 = 39 mu M and Log(10) GI(50) = -5.38. Our results suggest that these compounds are highly cytotoxic and cytostatic against human cancer cell lines.

引用

页码：255 / 259

页数：5

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