Combretastatin A-4顺式锁定衍生化研究进展

Progress in cis-Restricted Derivations of Combretastatin A-4

Combretastatin A-4(CA4)是天然抗肿瘤化合物,其顺式二苯乙烯构型对活性起关键作用。采用环状结构进行CA4的顺式构型锁定已成为目前结构改造的主要思路。本文从三元环、五元环、六元环锁定及骨架延伸锁定等方面综述了近年来CA4烯碳桥顺式锁定改造及衍生化的研究进展。

Combretastatin A-4 （CA4） is an important new generation vascular disrupting agent （VDA） from plant. The cis-stilbene configuration of which plays a crucial role on antitumor and anti-vascular activities. The ring formation in ethylene moiety has been considered to be the main idea for structure modification of CA4. The recent progress in cis-restricted derivations of CA4 representing by three, five, six-membered ring formation as well as skeleton extension has been reviewed.