Ying-Qian Liu1,2, Wen-Qun Li1, Susan L Morris-Natschke3, Keduo Qian3, Liu Yang4, Gao-Xiang Zhu1, Xiao-Bing Wu1, An-Liang Chen2, Shao-Yong Zhang2, Xiang Nan1, Kuo-Hsiung Lee3,5. 1. School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China. 2. Provincial Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Lin'an 311300, P. R. China. 3. Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599. 4. Environmental and Municipal Engineering School, Lanzhou Jiaotong University, Lanzhou, 730000, P. R. China. 5. Chinese Medicine Research and Development Center, China Medical University Hospital, Taichung, 40447, Taiwan.
Abstract
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.
Camptothecins (n class="Chemical">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.
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