title: Synthesis and structure-activity relationship studies of cytotoxic vinorelbine amide analogues.
abstract: A series of 3-demethoxycarbonyl-3-acylamide methyl vinorelbine derivatives (compounds 7a-7z) were designed, synthesized, and evaluated for their inhibition activities against human non-small cell lung cancer cell line (A549). Most of the amide derivatives exhibited potent cytotoxicity, with the size of the introduced substituents being the foremost factor in determining the resultant cytotoxic activity. Test results in vivo against nude mice bearing A549 xenografts indicated that 7y showed comparable activities compared to the parent NVB.
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, PR China.
authors.forename: Lingjun
authors.initials: L
authors.lastname: Hu
authors.forename: Weibin
authors.initials: W
authors.lastname: Song
authors.forename: Yuhui
authors.initials: Y
authors.lastname: Meng
authors.forename: Dean
authors.initials: D
authors.lastname: Guo
authors.forename: Xuan
authors.initials: X
authors.lastname: Liu
authors.forename: Lihong
authors.initials: L
authors.lastname: Hu
mesh_terms: D000577:Amides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D014747:Vinblastine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000077235:Vinorelbine
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D014747:Vinblastine; D000077235:Vinorelbine