The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
A novel series of [2.2.1]-azahydantoins has been designed and synthesized in an enantiospecific manner. The ability of these compounds to act as antagonists to the androgen receptor was investigated and several were found to have potent activity in vitro.
Balog
Aaron
A
Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. aaron.balog@bms.com
Salvati
Mark E
ME
Shan
Weifang
W
Mathur
Arvind
A
Leith
Leslie W
LW
Wei
Donna D
DD
Attar
Ricardo M
RM
Geng
Jieping
J
Rizzo
Cheryl A
CA
Wang
Chihuei
C
Krystek
Stanley R
SR
Tokarski
John S
JS
Hunt
John T
JT
Gottardis
Marco
M
Weinmann
Roberto
R
D059002:Androgen Receptor Antagonists; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D005069:Evaluation Studies as Topic; D006801:Humans; D006827:Hydantoins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D059002:Androgen Receptor Antagonists; D001372:Aza Compounds; D006827:Hydantoins