微管蛋白抑制剂Combretastatin A-4类似物的研究进展

摘要

微管蛋白在细胞生长、维持形态、信号传导及有丝分裂等过程中,均起着重要的作用.微管蛋白抑制剂是近年来热门的抗肿瘤药物.Combretastatin A-4 (CA-4)从南非灌木柳树皮Combretum caffrum树干中提取分离得到的二苯乙烯类化合物,是目前已知微管蛋白抑制剂中活性最强的化合物之一,但是也存在着众多缺陷.近年来围绕提高CA-4水溶性、保持顺式构型等衍生物的设计研究成为了热点.本文就CA-4的结构改造及类似物设计的研究进展进行综述.%Tubulin plays an important role in cell growth, morphological maintenance, signal transduction and mitotic process. Tubulin inhibitors are the popular antitumor drugs in recent years. Combretastatin A-4 ( CA-4) is one of the tubulin inhibitors, which is extracted and isolated from the Combretum caffrum in South African. It is one of the most active compounds with tubulin-inhibiting activity, but has many defects. Currently, researchers have designed other derivatives, focusing on how to improve the water solubility while keep the yield-configuration. In this article we reviewed the structure modification and the progress in CA-4 analogue design.