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Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Li, Hong-yu; Wang, Yan; Heap, Charles R; King, Chi-Hsin R; Mundla, Sreenivasa R; Voss, Matthew; Clawson, David K; Yan, Lei; Campbell, Robert M; Anderson, Bryan D; Wagner, Jill R; Britt, Karen; Lu, Ku X; McMillen, William T; Yingling, Jonathan M.
Afiliação
  • Li HY; Discovery Chemistry Research and Technology, Lilly Research Laboratory, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. li_hong-yu@lilly.com
J Med Chem ; 49(6): 2138-42, 2006 Mar 23.
Article em En | MEDLINE | ID: mdl-16539403
ABSTRACT
Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus TGF-beta RII and MLK-7 kinases. Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay.
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Base de dados: MEDLINE Assunto principal: Pirazóis / Pirróis / Benzimidazóis / Proteínas Serina-Treonina Quinases / Receptores de Fatores de Crescimento Transformadores beta / MAP Quinase Quinase Quinases Idioma: En Ano de publicação: 2006 Tipo de documento: Article
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PubMed Links

Base de dados: MEDLINE Assunto principal: Pirazóis / Pirróis / Benzimidazóis / Proteínas Serina-Treonina Quinases / Receptores de Fatores de Crescimento Transformadores beta / MAP Quinase Quinase Quinases Idioma: En Ano de publicação: 2006 Tipo de documento: Article