【文章名】Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications.
Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications.
作者
Li, Jie Jack;Iula, Donna M.;Nguyen, Maria N.;Hu, Lain-Yen;Dettling, Danielle;Johnson, Theodore R.;Du, Daniel Y.;Shanmugasundaram, Veerabahu;Van Camp, Jennifer A.;Wang, Zhi;Harter, William G.;Yue, Wen-Song;Boys, Mark L.;Wade, Kimberly J.;Drummond, Elena M.
[摘要]：4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile [PF-0998425, (I)] is a novel, nonsteroidal androgen receptor antagonist for sebum control and treatment of androgenetic alopecia. It is potent, selective, and active in vivo. The compd. is rapidly metabolized systemically, thereby reducing the risk of unwanted systemic side effects due to its primary pharmacol. PF-0998425 was tested neg. in the 3T3 NRU assay, validating the rationale that redn. of conjugation might reduce potential phototoxicity.
