title: Synthesis and cytotoxicity of 2alpha-amido docetaxel analogues.
abstract: Various 2-amido docetaxel analogues were prepared and evaluated for their cytotoxicities. Among them, m-methoxy and m-chlorobenzoylamido analogues were most active but not superior to docetaxel and paclitaxel, and D-seco analogues inactive. Change of 2-benzoate to 2-benzamide may not improve their activities to drug-resistant cell lines.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, PR China. wfang@imm.ac.cn
authors.forename: Wei-Shuo
authors.initials: WS
authors.lastname: Fang
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Hong-Yan
authors.initials: HY
authors.lastname: Liu
authors.forename: Shao-Feng
authors.initials: SF
authors.lastname: Xu
authors.forename: Liang
authors.initials: L
authors.lastname: Wang
authors.forename: Qi-Cheng
authors.initials: QC
authors.lastname: Fang
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077143:Docetaxel; D019008:Drug Resistance, Neoplasm; D020128:Inhibitory Concentration 50; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D043823:Taxoids; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D043823:Taxoids; D000077143:Docetaxel; D017239:Paclitaxel