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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Advances in Topoisomerase I-Targeting Agents, Camptothecin Analogues

Author(s): Dae-Kee Kim and Namkyu Lee

Volume 2, Issue 6, 2002

Page: [611 - 619] Pages: 9

DOI: 10.2174/1389557023405530

Price: $65

Abstract

The present review concentrates on camptothecin (CPT) analogues, the most extensively studied topoisomerase I (topo I) inhibitors, and provides concise information on the structural features of human topo I enzyme, mechanisms of interaction of CPT with topo I, structure-activity relationship study of CPT analogues including the influence of lactone stability on antitumor activity, and recent updates of valuable CPT analogues.

Keywords: topoisomerase, camptothecin, structural features of human topo enzyme, structure-activity relationship, monomeric protein, lurtotecan, rubitecan, highly lipophilic

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