Developments of Combretastatin A-4 Derivatives as Anticancer Agents

Y. Shan      Shan; J.      Zhang; Z.      Liu; M.      Wang; Y.      Dong

doi:10.2174/092986711794480221

Abstract

Tubulin protein is one of several members of a small family of globular proteins. It offers a potential target for anticancer drug design and development. Combretastatin A-4 (CA-4) is a potent anticancer and antiangiogenesis natural substance isolated from Combretum caffrum. Modifications on the CA-4 structure have led to a great number of novel CA-4 derivatives as potent tubulin inhibitors and high cytotoxic anticancer agents is becoming an interesting field, leading to a breakthrough in the treatment of cancer. In this review, the recent developments of novel CA-4 derivatives via the modifications on the A- and B-ring and the double bond as anticancer agents are discussed.

Keywords: Combretastatin A-4, Tubulin inhibitors, Anticancer, Antineoplastic Agents, Structure-Activity Relationships, antiangiogenesis, Combretum caffrum, chromo-somes, mitosis, microtu-bules, apoptosis, colchicine, vinca alka-loid domain, vinblastine, vincristine, Combretastatins, stilbenoid phenol, tubulin polymerization, chemotherapeutic, structure-activity relationship (SAR), human myelogenous leukaemia cell line, phosphate diesters, carcinoma, pinacolylboronate, boronic acid, Ethene Bridge, olefinic bridge, antineoplastic activity, hyperploid