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.
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.
Xiao
Hai-Yun
HY
Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA. haiyun.xiao@bms.com
Balog
Aaron
A
Attar
Ricardo M
RM
Fairfax
David
D
Fleming
Linda B
LB
Holst
Christian L
CL
Martin
Gregory S
GS
Rossiter
Lana M
LM
Chen
Jing
J
Cvjic
Mary-Ellen
ME
Dell-John
Janet
J
Geng
Jieping
J
Gottardis
Marco M
MM
Han
Wen-Ching
WC
Nation
Andrew
A
Obermeier
Mary
M
Rizzo
Cheryl A
CA
Schweizer
Liang
L
Spires
Thomas
T
Shan
Weifang
W
Gavai
Ashvinikumar
A
Salvati
Mark E
ME
Vite
Gregory
G
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
C410798:AR protein, human; D000970:Antineoplastic Agents; D009570:Nitriles; D011944:Receptors, Androgen; C014356:benzonitrile