Camptothecin: Roles of the D and E Rings in Binding to the Topoisomerase I-DNA Covalent Binary Complex

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Camptothecin: Roles of the D and E Rings in Binding to the Topoisomerase I-DNA Covalent Binary Complex

Anti-Cancer Agents in Medicinal Chemistry, 5(4): 353-362.

Author(s): S M Hecht.

Affiliation: Department of Chemistry,University of Virginia, Charlottesville, Virginia 22901, USA.


The alkaloid camptothecin is the prototypical DNA topoisomerase I poison. This core structure has formed the basis for two marketed antitumor agents and numerous clinical candidates, and has been the focus of many synthetic and medicinal chemistry studies. Recent reports have furthered our understanding of the roles played by the D and E rings of camptothecin in stabilization of the enzyme-DNA-camptothecin ternary complex. Important parameters for further study and optimization include the facility of E-ring lactone hydrolysis and the prospects for replacing the E ring with more stable structures, the role of the 14-CH group in binary complex binding, and the effect of ternary complex dynamics on the expression of cytotoxicity by the camptothecins.


topoisomerase I, camptothecin, cytotoxic agents, enzyme-dna covalent binary complex, luotonin a, antitumor agents.

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Article Details

Volume: 5
Issue Number: 4
First Page: 353
Last Page: 362
Page Count: 10
DOI: 10.2174/1568011054222373
Price: $58

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