title: The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening.
abstract: A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify compounds that exhibited in vivo potency equal to that of the marketed antiandrogen Casodex when orally administered.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development L.L.C., 666 Stockton Drive, Exton, PA 19341, USA. jlanter@prdus.jnj.com
authors.forename: James C
authors.initials: JC
authors.lastname: Lanter
authors.forename: James J
authors.initials: JJ
authors.lastname: Fiordeliso
authors.forename: Weiqin
authors.initials: W
authors.lastname: Jiang
authors.forename: George F
authors.initials: GF
authors.lastname: Allan
authors.forename: Muh-Tsann
authors.initials: MT
authors.lastname: Lai
authors.forename: Olivia
authors.initials: O
authors.lastname: Linton
authors.forename: Do Won
authors.initials: do W
authors.lastname: Hahn
authors.forename: Scott G
authors.initials: SG
authors.lastname: Lundeen
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000284:Administration, Oral; D000726:Androgen Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D059002:Androgen Receptor Antagonists; D000813:Anilides / Q000494:pharmacology; D000818:Animals; D004353:Drug Evaluation, Preclinical / Q000379:methods; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008297:Male; D009570:Nitriles / Q000494:pharmacology; D011467:Prostate / Q000187:drug effects*; D051381:Rats; D013329:Structure-Activity Relationship; D014105:Tosyl Compounds / Q000494:pharmacology
chemical_list: D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D000813:Anilides; D007211:Indoles; D009570:Nitriles; D014105:Tosyl Compounds; C053541:bicalutamide