title: beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model.
abstract: Through an in vivo screening model, we developed the in vivo SAR of beta-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development L.L.C., 665 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: Vernon C
authors.initials: VC
authors.lastname: Alford
authors.forename: Xuqing
authors.initials: X
authors.lastname: Zhang
authors.forename: Kenneth M
authors.initials: KM
authors.lastname: Wells
authors.forename: Ronald K
authors.initials: RK
authors.lastname: Russell
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: Scott
authors.initials: S
authors.lastname: Lundeen
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000284:Administration, Oral; D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004195:Disease Models, Animal; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D000432:Methanol / Q000031:analogs & derivatives* / Q000737:chemistry*; D051379:Mice; D009368:Neoplasm Transplantation; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000726:Androgen Antagonists; D000970:Antineoplastic Agents; D007211:Indoles; D000432:Methanol