Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

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. (C) 2012 Elsevier Ltd. All rights reserved.