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10.1021/ml900018m

http://scihub22266oqcxt.onion/10.1021/ml900018m
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suck abstract from ncbi


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pmid24900171
      ACS+Med+Chem+Lett 2010 ; 1 (1 ): 30-4
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  • Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295 #MMPMID24900171
  • Qian X ; McDonald A ; Zhou HJ ; Adams ND ; Parrish CA ; Duffy KJ ; Fitch DM ; Tedesco R ; Ashcraft LW ; Yao B ; Jiang H ; Huang JK ; Marin MV ; Aroyan CE ; Wang J ; Ahmed S ; Burgess JL ; Chaudhari AM ; Donatelli CA ; Darcy MG ; Ridgers LH ; Newlander KA ; Schmidt SJ ; Chai D ; Colón M ; Zimmerman MN ; Lad L ; Sakowicz R ; Schauer S ; Belmont L ; Baliga R ; Pierce DW ; Finer JT ; Wang Z ; Morgan BP ; Morgans DJ Jr ; Auger KR ; Sung CM ; Carson JD ; Luo L ; Hugger ED ; Copeland RA ; Sutton D ; Elliott JD ; Jackson JR ; Wood KW ; Dhanak D ; Bergnes G ; Knight SD
  • ACS Med Chem Lett 2010[Apr]; 1 (1 ): 30-4 PMID24900171 show ga
  • 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-hydroxyethyl]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 1 has demonstrated broad antitumor activity in vivo and is currently in human clinical trials.
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