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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.
Afiliação
  • 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 em 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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Receptores Proteína Tirosina Quinases / Inibidores de Proteínas Quinases Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Receptores Proteína Tirosina Quinases / Inibidores de Proteínas Quinases Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article