Department of Pharmacy, The First Affiliated Hospital of Medical College, Xi'an Jiaotong University, Xi'an, Shaanxi Province, 710061, PR China.
Curr Med Chem. 2011;18(4):523-38. doi: 10.2174/092986711794480221.
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.
微管蛋白是球形蛋白家族的几个成员之一。它为抗癌药物的设计和开发提供了一个潜在的目标。Combretastatin A-4（CA-4）是一种从 Combretum caffrum 中分离出来的强效抗癌和抗血管生成天然物质。CA-4 结构的修饰导致了大量新型 CA-4 衍生物作为有效的微管蛋白抑制剂和高细胞毒性抗癌剂，这成为一个有趣的领域，为癌症治疗带来了突破。在这篇综述中，讨论了通过对 A-和 B-环以及双键的修饰来开发新型 CA-4 衍生物作为抗癌剂的最新进展。
