title: The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
abstract: 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.
authors.affiliation: Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. aaron.balog@bms.com
authors.forename: Aaron
authors.initials: A
authors.lastname: Balog
authors.forename: Mark E
authors.initials: ME
authors.lastname: Salvati
authors.forename: Weifang
authors.initials: W
authors.lastname: Shan
authors.forename: Arvind
authors.initials: A
authors.lastname: Mathur
authors.forename: Leslie W
authors.initials: LW
authors.lastname: Leith
authors.forename: Donna D
authors.initials: DD
authors.lastname: Wei
authors.forename: Ricardo M
authors.initials: RM
authors.lastname: Attar
authors.forename: Jieping
authors.initials: J
authors.lastname: Geng
authors.forename: Cheryl A
authors.initials: CA
authors.lastname: Rizzo
authors.forename: Chihuei
authors.initials: C
authors.lastname: Wang
authors.forename: Stanley R
authors.initials: SR
authors.lastname: Krystek
authors.forename: John S
authors.initials: JS
authors.lastname: Tokarski
authors.forename: John T
authors.initials: JT
authors.lastname: Hunt
authors.forename: Marco
authors.initials: M
authors.lastname: Gottardis
authors.forename: Roberto
authors.initials: R
authors.lastname: Weinmann
mesh_terms: 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
chemical_list: D059002:Androgen Receptor Antagonists; D001372:Aza Compounds; D006827:Hydantoins