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Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui, Minna; Hao, Xiaolin; Shin, Youngsook; Cardozo, Mario; He, Xiao; Henne, Kirk; Suchomel, Julia; McCarter, John; McGee, Lawrence R; San Miguel, Tisha; Medina, Julio C; Mohn, Deanna; Tran, Thuy; Wannberg, Sharon; Wong, Jamie; Wong, Simon; Zalameda, Leeanne; Metz, Daniela; Cushing, Timothy D.
Afiliación
  • Bui M; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Hao X; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Shin Y; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Cardozo M; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • He X; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Henne K; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Suchomel J; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • McCarter J; Department of Therapeutic Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • McGee LR; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • San Miguel T; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • Medina JC; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Mohn D; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • Tran T; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Wannberg S; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • Wong J; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Wong S; Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
  • Zalameda L; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • Metz D; Department of Inflammation Research, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
  • Cushing TD; Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
Bioorg Med Chem Lett ; 25(5): 1104-9, 2015 Mar 01.
Article en En | MEDLINE | ID: mdl-25666823
ABSTRACT
2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good selectivity over three other class I PI3K isoforms. Some of those analogs showed favorable pharmacokinetic properties.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinolinas / Inhibidores de Proteínas Quinasas / Fosfatidilinositol 3-Quinasa Clase I Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Quinolinas / Inhibidores de Proteínas Quinasas / Fosfatidilinositol 3-Quinasa Clase I Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos