ANTINEOPLASTIC AGENTS .291. ISOLATION AND SYNTHESIS OF COMBRETASTATINS A-4, A-5, AND A-6
ANTINEOPLASTIC AGENTS .291. ISOLATION AND SYNTHESIS OF COMBRETASTATINS A-4, A-5, AND A-6
复制标题
DOI：
10.1021/jm00010a011
复制
发表时间：
1995-05-12
影响因子：
7.3
通讯作者：
HOGAN, F
中科院分区：
文献类型：
--
作者：
PETTIT, GR;SINGH, SB;HOGAN, F
研究了风车子Combretum caffrum（Eckl.和Zeyh）Kuntze（使君子科），一种原产于南非的物种进行了调查。随后，我们从C.咖啡。一些芪类化合物被证明是有效的抗有丝分裂剂，它们抑制微管蛋白聚合和秋水仙素与微管蛋白的结合。Combretastatin A-4已被证明是该系列中最有效的癌细胞生长抑制剂。目前，这种顺式芪是最有效的抑制剂秋水仙碱结合微管蛋白和最简单的天然产品，但描述了这种有效的抗微管蛋白的影响。还发现考布他汀A-4、A-5和A-6抑制淋病奈瑟菌的生长。已经描述了考布他汀A-4（2a）、A-5（2c）和A-6（3a）的分离和合成的细节。
The antineoplastic constituents of Combretum caffrum (Eckl. and Zeyh) Kuntze (Combretaceae family), a species indigenous to South Africa, have been investigated. Subsequently we isolated a series of closely related bibenzyls, stilbenes, and phenanthrenes from C. caffrum. Some of the stilbenes proved to be potent antimitotic agents which inhibited both tubulin polymerization and the binding of colchicine to tubulin. Combretastatin A-4 has been shown to be the most potent cancer cell growth inhibitor of the series. Presently this cis-stilbene is the most effective inhibitor of colchicine binding to tubulin and the simplest natural product yet described with such potent antitubulin effects. Combretastatin A-4, A-5, and A-6 were also found to inhibit growth of Neisseria gonorrhoeae. Details of the isolation and syntheses of combretastatins A-4 (2a), A-5 (2c), and A-6 (3a) have been described.