Journal
MEDICINAL RESEARCH REVIEWS
Volume 35, Issue 4, Pages 753-789Publisher
WILEY
DOI: 10.1002/med.21342
Keywords
camptothecins; DNA topoisomerase I; biological activities; structure-activity relationship
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Funding
- National Natural Science Foundation of China [30800720, 31371975]
- Fundamental Research Funds for the Central Universities [lzujbky-2014-k19]
- Foundation of Priority Forestry Disciplines in Zhejiang AF University [KF201325]
- NIH from the National Cancer Institute [CA177584]
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Camptothecins (CPTs) are cytotoxic natural alkaloids that specifically target DNA topoisomerase I. Research on CPTs has undergone a significant evolution from the initial discovery of CPT in the late 1960s through the study of synthetic small-molecule derivatives to investigation of macromolecular constructs and formulations. Over the past years, intensive medicinal chemistry efforts have generated numerous CPT derivatives. Three derivatives, topotecan, irinotecan, and belotecan, are currently prescribed as anticancer drugs, and several related compounds are now in clinical trials. Interest in other biological effects, besides anticancer activity, of CPTs is also growing exponentially, as indicated by the large number of publications on the subject during the last decades. Therefore, the main focus of the present review is to provide an ample but condensed overview on various biological activities of CPT derivatives, in addition to continued up-to-date coverage of anticancer effects. (C) 2014 Wiley Periodicals, Inc.
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