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Powell, Noel A.; Hoffman, Jennifer K.; Ciske, Fred L.; Kaufman, Michael D.; Kohrt, Jeffrey T.; Quin, John; Sheehan, Derek J.; Delaney, Amy; Baxi, Sangita M.; Catana, Cornel; McConnell, Patrick; Ohren, Jeff; Perrin, Lisa A.; Edmunds, Jeremy J.
Bioorganic & medicinal chemistry letters, 02/2013, Letnik: 23, Številka: 4Journal Article
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. 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.
