Synthesis and cytotoxicity of 2alpha-amido docetaxel analogues.
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.
Fang
Wei-Shuo
WS
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
Liu
Ying
Y
Liu
Hong-Yan
HY
Xu
Shao-Feng
SF
Wang
Liang
L
Fang
Qi-Cheng
QC
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
D000972:Antineoplastic Agents, Phytogenic; D043823:Taxoids; D000077143:Docetaxel; D017239:Paclitaxel