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[摘要]：Inhibition of mitotic kinesins represents a novel approach for the discovery of a new generation of anti-mitotic cancer chemotherapeutics We report here the discovery of the first potent and selective inhibitor of centromere-associated protein E (CENP-E) 3-chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxy ethyl]imidazo[1.2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl )oxy]benzamide (GSK923295: 1), starting from a high-throughput screening hit, 3-chloro-4-isopropoxybenzoic acid 2 Compound I has demonstrated broad antitumor activity in vivo and is currently in human clinical trials. |
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