Discovery of diarylhydantoins as new selective androgen receptor modulators

…, C Robin-Jagerschmidt…

文献索引：Nique, Francois; Hebbe, Severine; Peixoto, Christophe; Annoot, Denis; Lefrancois, Jean-Michel; Duval, Eric; Michoux, Laurence; Triballeau, Nicolas; Lemoullec, Jean-Michel; Mollat, Patrick; Minet, Dominique; Clement-Lacroix, Philippe; Robin-Jagerschmidt, Catherine; Fleury, Damien; Guedin, Denis; Deprez, Pierre; Thauvin, Maxime; Prange, Thierry Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8225 - 8235,11 Title/Abstract Full Text Show Details Nique, Francois; Hebbe, Severine; Peixoto, Christophe; Annoot, Denis; Lefrancois, Jean-Michel; Duval, Eric; Michoux, Laurence; Triballeau, Nicolas; Lemoullec, Jean-Michel; Mollat, Patrick; Thauvin, Maxime; Prange, Thierry; Minet, Dominique; Clement-Lacroix, Philippe; Robin-Jagerschmidt, Catherine; Fleury, Damien; Guedin, Denis; Deprez, Pierre Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8225 - 8235

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被引用次数: 22

摘要

A novel selective androgen receptor modulator scaffold has been discovered through structural modifications of hydantoin antiandrogens. Several 4-(4-hydroxyphenyl)-N- arylhydantoins displayed partial agonism with nanomolar in vitro potency in transactivation experiments using androgen receptor (AR) transfected cells. In a standard castrated male rat model, several compounds showed good anabolic activity on levator ani muscle, ...