美车霉素A类似物的合成及其抗肿瘤活性

Synthesis and antitumor activity of mechercharmycin A analogues.

作者信息

Hernández Delia, Altuna Marta, Cuevas Carmen, Aligué Rosa, Albericio Fernando, Alvarez Mercedes

机构信息

Institute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri Reixac 10, E-08028 Barcelona, Spain.

出版信息

J Med Chem. 2008 Sep 25;51(18):5722-30. doi: 10.1021/jm800513w.

DOI:10.1021/jm800513w

PMID:18763756

Abstract

Several analogues of the cytotoxic thiopeptide IB-01211 or mechercharmycin A (1) have been synthesized. The cytotoxicity of 1 and the synthesized analogues were evaluated against a panel of three human tumor cell lines. Thiopeptide 1 and the most active derivatives 2 and 3c were chosen for further studies on effects on cell cycle progression and induction of apoptosis. Interestingly, the inhibition of cell division and activation of a programmed cell death by apoptosis were detected.

摘要

已经合成了细胞毒性硫肽IB - 01211或美切霉素A（1）的几种类似物。针对一组三种人类肿瘤细胞系评估了1以及合成类似物的细胞毒性。选择硫肽1以及活性最高的衍生物2和3c进一步研究其对细胞周期进程的影响和诱导凋亡的作用。有趣的是，检测到细胞分裂受到抑制以及通过凋亡激活程序性细胞死亡。