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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.
Huang, Audris; Jayaraman, Lata; Fura, Aberra; Vite, Gregory D; Trainor, George L; Gottardis, Marco M; Spires, Thomas E; Spires, Vanessa M; Rizzo, Cheryl A; Obermeier, Mary T; Elzinga, Paul A; Todderud, Gordon; Fan, Yi; Newitt, John A; Beyer, Sophie M; Zhu, Yongxin; Warrack, Bethanne M; Goodenough, Angela K; Tebben, Andrew J; Doweyko, Arthur M; Gold, David L; Balog, Aaron.
Affiliation
  • Huang A; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Jayaraman L; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Fura A; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Vite GD; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Trainor GL; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Gottardis MM; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Spires TE; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Spires VM; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Rizzo CA; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Obermeier MT; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Elzinga PA; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Todderud G; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Fan Y; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Newitt JA; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Beyer SM; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Zhu Y; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Warrack BM; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Goodenough AK; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Tebben AJ; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Doweyko AM; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Gold DL; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
  • Balog A; Bristol-Myers Squibb Research and Development , Princeton, New Jersey 08543-4000, United States.
ACS Med Chem Lett ; 7(1): 40-5, 2016 Jan 14.
Article de En | MEDLINE | ID: mdl-26819663
ABSTRACT
Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the treatment of castration-resistant prostate cancer (CRPC) culminated in the discovery of BMS-351 (compound 18), a pyridyl biaryl benzimidazole with an excellent in vivo profile. Biological evaluation of BMS-351 at a dose of 1.5 mg in castrated cynomolgus monkeys revealed a remarkable reduction in testosterone levels with minimal glucocorticoid and mineralcorticoid perturbation. Based on a favorable profile, BMS-351 was selected as a candidate for further preclinical evaluation.
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Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Langue: En Journal: ACS Med Chem Lett Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique
Texte intégral
Ajouter à My VHL
Imprimer
XML
PubMed Links
Recherche sur Google

Texte intégral: 1 Collection: 01-internacional Base de données: MEDLINE Langue: En Journal: ACS Med Chem Lett Année: 2016 Type de document: Article Pays d'affiliation: États-Unis d'Amérique