title: Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
abstract: A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo.
authors.affiliation: Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA. haiyun.xiao@bms.com
authors.forename: Hai-Yun
authors.initials: HY
authors.lastname: Xiao
authors.forename: Aaron
authors.initials: A
authors.lastname: Balog
authors.forename: Ricardo M
authors.initials: RM
authors.lastname: Attar
authors.forename: David
authors.initials: D
authors.lastname: Fairfax
authors.forename: Linda B
authors.initials: LB
authors.lastname: Fleming
authors.forename: Christian L
authors.initials: CL
authors.lastname: Holst
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Martin
authors.forename: Lana M
authors.initials: LM
authors.lastname: Rossiter
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Mary-Ellen
authors.initials: ME
authors.lastname: Cvjic
authors.forename: Janet
authors.initials: J
authors.lastname: Dell-John
authors.forename: Jieping
authors.initials: J
authors.lastname: Geng
authors.forename: Marco M
authors.initials: MM
authors.lastname: Gottardis
authors.forename: Wen-Ching
authors.initials: WC
authors.lastname: Han
authors.forename: Andrew
authors.initials: A
authors.lastname: Nation
authors.forename: Mary
authors.initials: M
authors.lastname: Obermeier
authors.forename: Cheryl A
authors.initials: CA
authors.lastname: Rizzo
authors.forename: Liang
authors.initials: L
authors.lastname: Schweizer
authors.forename: Thomas
authors.initials: T
authors.lastname: Spires
authors.forename: Weifang
authors.initials: W
authors.lastname: Shan
authors.forename: Ashvinikumar
authors.initials: A
authors.lastname: Gavai
authors.forename: Mark E
authors.initials: ME
authors.lastname: Salvati
authors.forename: Gregory
authors.initials: G
authors.lastname: Vite
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D008297:Male; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D011471:Prostatic Neoplasms / Q000188:drug therapy; D011944:Receptors, Androgen / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C410798:AR protein, human; D000970:Antineoplastic Agents; D009570:Nitriles; D011944:Receptors, Androgen; C014356:benzonitrile