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Bioorganic & Medicinal Chemistry

Bioorganic & Medicinal Chemistry

IF: 3.3
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Camptothecin: current perspectives

Published:1 April 2004 DOI: 10.1016/j.bmc.2003.11.036 PMID: 15028252
Craig J. Thomas, Nicolas J. Rahier, Sidney M. Hecht

Abstract

This review provides a detailed discussion of recent advances in the medicinal chemistry of camptothecin, a potent antitumor antibiotic. Two camptothecin analogues are presently approved for use in the clinic as antitumor agents and several others are in clinical trials. Camptothecin possesses a novel mechanism of action involving the inhibition of DNA relaxation by DNA topoisomerase I, and more specifically the stabilization of a covalent binary complex formed between topoisomerase I and DNA. This review summarizes the current status of studies of the mechanism of action of camptothecin, including topoisomerase I inhibition and additional cellular responses. Modern synthetic approaches to camptothecin and several of the semi-synthetic methods are also discussed. Finally, a systematic evaluation of novel and important analogues of camptothecin and their contribution to the current structure–activity profile are considered.

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Procduct Name CAS Molecular Formula Supplier Price
(+)-Camptothecin 7689-03-4 C20H16N2O4 747 suppliers $9.00-$1900.44
TOPOISOMERASE I 80449-01-0 C20H27N3O 45 suppliers Inquiry
Camptothecin 119403-33-7 C20H14N2O4 16 suppliers Inquiry

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