Pettit G R, Singh S B, Boyd M R, Hamel E, Pettit R K, Schmidt J M, Hogan F
Cancer Research Institute, Arizona State University, Tempe 85287-1604, USA.
J Med Chem. 1995 May 12;38(10):1666-72. doi: 10.1021/jm00010a011.
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.
南非本土植物南非风车子（使君子科）的抗肿瘤成分已得到研究。随后我们从南非风车子中分离出了一系列密切相关的联苄、芪类化合物和菲类化合物。一些芪类化合物被证明是有效的抗有丝分裂剂，可抑制微管蛋白聚合以及秋水仙碱与微管蛋白的结合。康普瑞他汀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，这种顺式芪是秋水仙碱与微管蛋白结合的最有效抑制剂，也是迄今所描述的具有如此强大抗微管蛋白作用的最简单天然产物。康普瑞他汀A - 4、A - 5和A - 6还被发现可抑制淋病奈瑟菌的生长。康普瑞他汀A - 4（2a）、A - 5（2c）和A - 6（3a）的分离和合成细节已有描述。
