1421367-64-7Relevant academic research and scientific papers
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase
Powell, Noel A.,Hoffman, Jennifer K.,Ciske, Fred L.,Kaufman, Michael D.,Kohrt, Jeffrey T.,Quin III, John,Sheehan, Derek J.,Delaney, Amy,Baxi, Sangita M.,Catana, Cornel,McConnell, Patrick,Ohren, Jeff,Perrin, Lisa A.,Edmunds, Jeremy J.
, p. 1046 - 1050 (2013/03/14)
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase
Powell, Noel A.,Hoffman, Jennifer K.,Ciske, Fred L.,Kohrt, Jeffrey T.,Baxi, Sangita M.,Peng, Yun-Wen,Zhong, Min,Catana, Cornel,Ohren, Jeff,Perrin, Lisa A.,Edmunds, Jeremy J.
, p. 1051 - 1055 (2013/03/13)
Optimization of the ADME properties of a series of 2,4-diaminopyrimidine-5- carboxamide inhibitors of Sky kinase resulted in the identification of highly selective compounds with properties suitable for use as in vitro and in vivo tools to probe the effects of Sky inhibition.
