Combretastatin A-4及其类似物构效关系研究进展

Research progress in the structure-activity relationship of combretastatin A-4 and its analogues

Combretastatin A-4(CA-4)是一个天然的秋水仙碱结合位点抑制剂,其突出的生物活性引起人们的高度关注,近年来,不断有结构多样的类似物被发现。这些类似物主要是针对CA-4的A环、B环和顺式双键的结构修饰,其中,以用单原子或环状结构替代顺式双键进而保持A/B环具有合适的空间距离和角度为主。本文对CA-4及其类似物构效关系的研究进行简单概述。

Combretastatin A-4 （CA-4）, as a natural colchicine binding site inhibitor, has prominent biological activity, which has aroused widespread attention. In last two decades, a large number of analogues of CA-4 have been reported with significant structural diversity. These analogues are mainly about the modifications of the ring A, ring B and cis-double bond. Among them, replacement the cis-double bond with single atom or cyclic structure to make sure the suitable distance between ring A and ring B is a simple and effective stratagy of modifications about CA-4. A synopsis of recent advances in research of structure-activity relationship of CA-4 and its analogues were reviewed.