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), a natural inhibitor of colchicine-binding site, has drawn great attention for its outstanding biological activity. In recent years, many structural analogs have been found. These analogs are mainly directed toward the structural modification of the A ring, the B ring and the cis double bond of CA-4 in which the substitution of the cis double bond by a monoatomic or cyclic structure to keep the A / B ring at an appropriate spatial distance and Main point of view. This article briefly reviews the structure-activity relationship of CA-4 and its analogs.