喜树碱结构修饰研究进展

Research progress in structural modification of Camptothecins

摘要:

喜树碱及其衍生物是一类具有广谱抗肿瘤活性的生物碱，对恶性肿瘤具有显著抑制作用，已开发出伊立替康、 拓扑替康等临床用药。喜树碱类抗肿瘤药物的主要缺陷是水溶解度低、结构稳定性差、毒副作用强，因而相应的结构修饰策略也随着药物开发的进程而逐渐迭代。作者以提高喜树碱类抗肿瘤药物药效为目的，从结构修饰策略角度综述喜树碱及其衍生物的发展过程，着重总结2015年以来在各种策略指导下喜树碱类衍生物研究的最新进展，为后期喜树碱类抗肿瘤新药物的开发提供参考。

Abstract:

Camptothecin and its derivatives are alkaloids with broad-spectrum anti-tumor activities and have significant inhibitory effect on malignant tumors. Its derivatives such as irinotecan and topotecan have been on market over 20 years. As a antitumor drug family, main problems of camptothecins are low solubility, poor structural stability, and strong toxic side effects, therefore the corresponding structural modification strategies are upgraded with the improvement of drug development. The author aims to improve the efficacy of camptothecin based anti-tumor drugs and reviews the development process of camptothecin and its derivatives from the perspective of structural modification strategies. The focus is on summarizing the latest progress in research on camptothecin based derivatives under various strategic guidance since 2015, providing reference for the development of new camptothecin based anti-tumor drugs in the future.