Perspectives on Biologically Active Camptothecin Derivatives

• Published in: Medicinal research reviews Vol. 35; no. 4; pp. 753 - 789
• Main Authors: Liu, Ying-Qian, Li, Wen-Qun, Morris-Natschke, Susan L., Qian, Keduo, Yang, Liu, Zhu, Gao-Xiang, Wu, Xiao-Bing, Chen, An-Liang, Zhang, Shao-Yong, Nan, Xiang, Lee, Kuo-Hsiung
• Format: Journal Article
• Language: English
• Published: United States Blackwell Publishing Ltd 01.07.2015; Wiley Subscription Services, Inc
• Subjects: Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; biological activities; Camptothecin - chemistry; Camptothecin - pharmacology; camptothecins; DNA topoisomerase I; Humans; Pharmaceutical industry; structure-activity relationship; biological activities; camptothecins; structure-activity relationship; DNA topoisomerase I
• ISSN: 0198-6325; 1098-1128; 1098-1128
• DOI: 10.1002/med.21342

Camptothecins (CPTs) are cytotoxic natural alkaloids that specifically target DNA topoisomerase I. Research on CPTs has undergone a significant evolution from the initial discovery of CPT in the late 1960s through the study of synthetic small‐molecule derivatives to investigation of macromolecular constructs and formulations. Over the past years, intensive medicinal chemistry efforts have generated numerous CPT derivatives. Three derivatives, topotecan, irinotecan, and belotecan, are currently prescribed as anticancer drugs, and several related compounds are now in clinical trials. Interest in other biological effects, besides anticancer activity, of CPTs is also growing exponentially, as indicated by the large number of publications on the subject during the last decades. Therefore, the main focus of the present review is to provide an ample but condensed overview on various biological activities of CPT derivatives, in addition to continued up‐to‐date coverage of anticancer effects.