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Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.

ABSTRACT: 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.

SUBMITTER: Qian X 

PROVIDER: S-EPMC4007900 | biostudies-literature | 2010 Apr

REPOSITORIES: biostudies-literature

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Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.

Qian Xiangping X   McDonald Andrew A   Zhou Han-Jie HJ   Adams Nicholas D ND   Parrish Cynthia A CA   Duffy Kevin J KJ   Fitch Duke M DM   Tedesco Rosanna R   Ashcraft Luke W LW   Yao Bing B   Jiang Hong H   Huang Jennifer K JK   Marin Melchor V MV   Aroyan Carrie E CE   Wang Jianchao J   Ahmed Seyed S   Burgess Joelle L JL   Chaudhari Amita M AM   Donatelli Carla A CA   Darcy Michael G MG   Ridgers Lance H LH   Newlander Ken A KA   Schmidt Stanley J SJ   Chai Deping D   Colón Mariela M   Zimmerman Michael N MN   Lad Latesh L   Sakowicz Roman R   Schauer Stephen S   Belmont Lisa L   Baliga Ramesh R   Pierce Daniel W DW   Finer Jeffrey T JT   Wang Zhengping Z   Morgan Bradley P BP   Morgans David J DJ   Auger Kurt R KR   Sung Chiu-Mei CM   Carson Jeff D JD   Luo Lusong L   Hugger Erin D ED   Copeland Robert A RA   Sutton David D   Elliott John D JD   Jackson Jeffrey R JR   Wood Kenneth W KW   Dhanak Dashyant D   Bergnes Gustave G   Knight Steven D SD  

ACS medicinal chemistry letters 20100119 1

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-isopropoxyben  ...[more]

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