A-4诱导微管蛋白聚合抑制剂的最新进展

Title:Recent Advances in Combretastatin A-4 Inspired Inhibitors of Tubulin Polymerization: An Update

Volume: 29 Issue: 20

关键词: 康布他他汀A-4，微管，癌症，药物开发，微管蛋白聚合抑制剂，MTAS。

摘要: Cancer is one of the leading causes of fatality and mortality worldwide. Investigations on developing therapeutic strategies for cancer are supported throughout the world. The massive achievements in molecular sciences involving biochemistry, molecular chemistry, medicine, and pharmacy, and high throughput techniques such as genomics and proteomics have helped create new potential drug targets for cancer treatment. Microtubules are very attractive targets for cancer therapy because of the crucial roles they play in cell division. In recent years, lots of efforts have been put into the identification of new microtubule-targeting agents (MTAs) in anticancer therapy. Combretastatin A-4 (CA-4) is a natural compound that binds to microtubules’ colchicine binding site and inhibits microtubule polymerization. Due to CA-4’s structural simplicity, many analogs have been synthesized. This article summarises the new molecule development efforts to reach CA-4 analogues by pharmacophore group modifications, which have been reported since 2015.

Cite this article as:

Recent Advances in Combretastatin A-4 Inspired Inhibitors of Tubulin Polymerization: An Update, Current Medicinal Chemistry 2022; 29 (20) . https://dx.doi.org/10.2174/1871526522666220105114437