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Current Medicinal Chemistry

Volume 13 Issue 17
ISSN: 0929-8673
eISSN: 1875-533X

 

   All Titles

  Review Camptothecin: Current Perspectives
  pp.2021-2039 (19) Authors: Qing-Yong Li, Yuan-Gang Zu, Rong-Zhen Shi, Li-Ping Yao
 
 
      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
  Affiliation: Key Laboratory of Forest Plant Ecology (Northeast Forestry University), Ministry of Education,Harbin 150040, China.
 
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