Review Camptothecin: Current Perspectives

Author(s): Qing-Yong Li, Yuan-Gang Zu, Rong-Zhen Shi, Li-Ping Yao

Journal Name: Current Medicinal Chemistry

Volume 13 , Issue 17 , 2006

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The review provides a detailed discussion of recent advances in the medicinal chemistry of camptothecin, a potent antitumor agent that targets topoisomerase I. Thousands of CPT derivatives have been synthesized. Two of them, Topotecan and Irinotecan, are commercially approved for use in clinic as antitumor agents while more are still in clinic trials. This review summarizes the current status of the modern synthetic approaches to CPT, the mechanism of action of CPT, the structure-activity relationship(SAR), a number of novel CPT analogs and their biologic activity. There is a systematic evaluation of A-, B- and E-ring- modified camptothecins reported recently.

Keywords: Camptothecin, Antitumor, Topo I inhibitor

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Article Details

Year: 2006
Page: [2021 - 2039]
Pages: 19
DOI: 10.2174/092986706777585004

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