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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, John; Sheehan, Derek J; Delaney, Amy; Baxi, Sangita M; Catana, Cornel; McConnell, Patrick; Ohren, Jeff; Perrin, Lisa A; Edmunds, Jeremy J.
Affiliation
  • Powell NA; Pfizer Global Research & Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. napowell@comcast.net
Bioorg Med Chem Lett ; 23(4): 1046-50, 2013 Feb 15.
Article in En | MEDLINE | ID: mdl-23312472
ABSTRACT
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.
Subject(s)

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Receptor Protein-Tyrosine Kinases / Protein Kinase Inhibitors Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Document type: Article Affiliation country: United States

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Receptor Protein-Tyrosine Kinases / Protein Kinase Inhibitors Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Document type: Article Affiliation country: United States