title: Design and one-pot synthesis of new 7-acyl camptothecin derivatives as potent cytotoxic agents.
abstract: New 7-acyl camptothecin derivatives were designed and synthesized from camptothecin in a one-pot reaction through a Minisci type-reaction and were evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB, and KB-vin. All of the new compounds showed significant inhibition of human tumor cell growth, with IC(50) values ranging from 0.01538 to 13.342 μM. Most of the derivatives were more cytotoxic than irinotecan, and the (7a) and 7-propionyl (7b) analogs exhibited the highest cytotoxic activity against the tumor cell lines tested. This compound class merits further development as anticancer clinical trial candidates.
authors.affiliation: School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China. yqliu@lzu.edu.cn
authors.forename: Ying-Qian
authors.initials: YQ
authors.lastname: Liu
authors.forename: Wei
authors.initials: W
authors.lastname: Dai
authors.forename: Chih-Ya
authors.initials: CY
authors.lastname: Wang
authors.forename: Susan L
authors.initials: SL
authors.lastname: Morris-Natschke
authors.forename: Xing-Wen
authors.initials: XW
authors.lastname: Zhou
authors.forename: Liu
authors.initials: L
authors.lastname: Yang
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Yang
authors.forename: Wen-Qun
authors.initials: WQ
authors.lastname: Li
authors.forename: Kuo-Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D007624:KB Cells; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002166:Camptothecin