Abstract
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
Current Medicinal Chemistry
Title: Review Camptothecin: Current Perspectives
Volume: 13 Issue: 17
Author(s): Qing-Yong Li, Yuan-Gang Zu, Rong-Zhen Shi and Li-Ping Yao
Affiliation:
Keywords: Camptothecin, Antitumor, Topo I inhibitor
Abstract: 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.
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Cite this article as:
Li Qing-Yong, Zu Yuan-Gang, Shi Rong-Zhen and Yao Li-Ping, Review Camptothecin: Current Perspectives, Current Medicinal Chemistry 2006; 13 (17) . https://dx.doi.org/10.2174/092986706777585004
DOI https://dx.doi.org/10.2174/092986706777585004 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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