微管蛋白抑制剂Combretastatin A-4类似物的研究进展  

Research progress in derivatives of the tubulin inhibitor combretastatin A-4

作　　者：许勤龙[1] 周鹏[1] 李家明[1] 张恩立[1] 叶文峰[1] 

机构地区：[1]安徽中医学院药学院,安徽省现代中药重点实验室,合肥230031

出　　处：《中国新药杂志》2013年第3期301-306,318,共7页Chinese Journal of New Drugs

基　　金：安徽省自然科学基金(1208085MH128)

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.

关 键 词：微管蛋白抑制剂 衍生物 结构改造 

分 类 号：R979.1[医药卫生—药品]