Research progress in structural modification of Camptothecins

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.

Keywords

• camptothecin
• structural modification
• anti-tumor