Identification of a 4-(hydroxymethyl) diarylhydantoin as a selective androgen receptor modulator

…, C Housseman, H Klaassen, K Van Beeck…

文献索引：Nique, Francois; Hebbe, Severine; Triballeau, Nicolas; Peixoto, Christophe; Lefrancois, Jean-Michel; Jary, Helene; Alvey, Luke; Manioc, Murielle; Housseman, Christopher; Klaassen, Hugo; Van Beeck, Kris; Guedin, Denis; Namour, Florence; Minet, Dominque; Van Der Aar, Ellen; Feyen, Jean; Fletcher, Stephen; Blanque, Roland; Robin-Jagerschmidt, Catherine; Deprez, Pierre Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8236 - 8247,12 Title/Abstract Full Text Show Details Nique, Francois; Hebbe, Severine; Triballeau, Nicolas; Peixoto, Christophe; Lefrancois, Jean-Michel; Jary, Helene; Alvey, Luke; Manioc, Murielle; Housseman, Christopher; Klaassen, Hugo; Van Beeck, Kris; Guedin, Denis; Namour, Florence; Minet, Dominque; Van Der Aar, Ellen; Feyen, Jean; Fletcher, Stephen; Blanque, Roland; Robin-Jagerschmidt, Catherine; Deprez, Pierre Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8236 - 8247

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被引用次数: 18

摘要

Structural modification performed on a 4-methyl-4-(4-hydroxyphenyl) hydantoin series is described which resulted in the development of a new series of 4-(hydroxymethyl) diarylhydantoin analogues as potent, partial agonists of the human androgen receptor. This led to the identification of (S)-(−)-4-(4-(hydroxymethyl)-3-methyl-2, 5-dioxo-4- phenylimidazolidin-1-yl)-2-(trifluoromethyl) benzonitrile ((S)-(−)-18a, GLPG0492) ...