Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
J Med Chem
; 54(21): 7693-704, 2011 Nov 10.
Article
in En
| MEDLINE
| ID: mdl-21936524
ABSTRACT
An aryloxy tetramethylcyclobutane was identified as a novel template for androgen receptor (AR) antagonists via cell-based high-throughput screening. Follow-up to the initial "hit" established 5 as a viable lead. Further optimization to achieve full AR antagonism led to the discovery of 26 and 30, both of which demonstrated excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazoles
/
Bridged Bicyclo Compounds, Heterocyclic
/
Cyclobutanes
/
Androgen Antagonists
/
Antineoplastic Agents
Limits:
Animals
/
Humans
/
Male
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2011
Document type:
Article
Affiliation country:
United States