1.
J Med Chem
; 54(21): 7693-704, 2011 Nov 10.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21936524
RESUMO
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.