603301-06-0Relevant academic research and scientific papers
The development of potent and selective bisarylmaleimide GSK3 inhibitors
Engler, Thomas A.,Malhotra, Sushant,Burkholder, Timothy P.,Henry, James R.,Mendel, David,Porter, Warren J.,Furness, Kelly,Diefenbacher, Clive,Marquart, Angela,Reel, Jon K.,Li, Yihong,Clayton, Joshua,Cunningham, Brian,McLean, Johnathan,O'Toole, John C.,Brozinick, Joseph,Hawkins, Eric,Misener, Elizabeth,Briere, Daniel,Brier, Richard A.,Wagner, Jill R.,Campbell, Robert M.,Anderson, Bryan D.,Vaughn, Renee,Bennett, Donald B.,Meier, Timothy I.,Cook, James A.
, p. 899 - 903 (2007/10/03)
Many 3-aryl-4-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl) maleimides exhibit potent GSK3 inhibitory activity (50), although few show significant selectivity (>100 ×) versus CDK2, CDK4, or PKCβII. However, combining 3-(imidazo[1,2-a]pyridin-3-yl), 3-(pyrazolo[1,5-a]pyridin-3-yl) or aza-analogs with a 4-(2-acyl-(1,2,3,4- tetrahydro[1,4]diazepino[6,7,1-hi]indol -7-yl)) group on the maleimide resulted in very potent inhibitors of GSK3 (≤5 nM) with >160 to >10,000-fold selectivity versus CDK2/4 and PKCβII. These compounds also inhibited tau phosphorylation in cells and were effective in lowering plasma glucose in a rat model of type 2 diabetes (ZDF rat).
PURINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 39, (2008/06/13)
The present invention provides kinase inhibitors of Formula I.
