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Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Unwalla, Ray; Mousseau, James J; Fadeyi, Olugbeminiyi O; Choi, Chulho; Parris, Kevin; Hu, Baihua; Kenney, Thomas; Chippari, Susan; McNally, Christopher; Vishwanathan, Karthick; Kilbourne, Edward; Thompson, Catherine; Nagpal, Sunil; Wrobel, Jay; Yudt, Matthew; Morris, Carl A; Powell, Dennis; Gilbert, Adam M; Chekler, Eugene L Piatnitski.
Afiliación
  • Unwalla R; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Mousseau JJ; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Fadeyi OO; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Choi C; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Parris K; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Hu B; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Kenney T; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Chippari S; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • McNally C; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Vishwanathan K; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Kilbourne E; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Thompson C; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Nagpal S; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Wrobel J; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Yudt M; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Morris CA; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Powell D; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Gilbert AM; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
  • Chekler ELP; Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
J Med Chem ; 60(14): 6451-6457, 2017 07 27.
Article en En | MEDLINE | ID: mdl-28696695
In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of 7, and further insights from modeling studies of ligand receptor interactions are also presented.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirroles / Receptores Androgénicos / Anabolizantes / Andrógenos / Nitrilos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirroles / Receptores Androgénicos / Anabolizantes / Andrógenos / Nitrilos Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos