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Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.
J Med Chem ; 52(14): 4380-90, 2009 Jul 23.
Article em En | MEDLINE | ID: mdl-19555113
Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure-activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one (1) to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (42), a potent ATP mimetic inhibitor of Cdc7 kinase with IC(50) value of 7 nM, is also reported.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Proteínas Serina-Treonina Quinases / Proteínas de Ciclo Celular / Inibidores de Proteínas Quinases Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Piridinas / Proteínas Serina-Treonina Quinases / Proteínas de Ciclo Celular / Inibidores de Proteínas Quinases Idioma: En Ano de publicação: 2009 Tipo de documento: Article