title: Perspectives on biologically active camptothecin derivatives.
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.
authors: School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China.|Provincial Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Lin'an 311300, P. R. China.
authors: Ying-Qian
authors: YQ
authors: Liu
authors: School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China.
authors: Wen-Qun
authors: WQ
authors: Li
authors: Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599.
authors: Susan L
authors: SL
authors: Morris-Natschke
authors: Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599.
authors: Keduo
authors: K
authors: Qian
authors: Environmental and Municipal Engineering School, Lanzhou Jiaotong University, Lanzhou, 730000, P. R. China.
authors: Liu
authors: L
authors: Yang
authors: School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China.
authors: Gao-Xiang
authors: GX
authors: Zhu
authors: School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China.
authors: Xiao-Bing
authors: XB
authors: Wu
authors: Provincial Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Lin'an 311300, P. R. China.
authors: An-Liang
authors: AL
authors: Chen
authors: Provincial Engineering Laboratory of Biopesticide Preparation, Zhejiang A&F University, Lin'an 311300, P. R. China.
authors: Shao-Yong
authors: SY
authors: Zhang
authors: School of Pharmacy, Lanzhou University, Lanzhou 730000, P. R. China.
authors: Xiang
authors: X
authors: Nan
authors: Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599.|Chinese Medicine Research and Development Center, China Medical University Hospital, Taichung, 40447, Taiwan.
authors: Kuo-Hsiung
authors: KH
authors: Lee
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D002166:Camptothecin
keywords: DNA topoisomerase I; biological activities; camptothecins; structure-activity relationship