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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 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.