Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer.
Bioorg Med Chem Lett
; 21(18): 5442-5, 2011 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-21782422
ABSTRACT
Chemical starting points were investigated for downregulation of the androgen receptor as an approach to treatment of advanced prostate cancer. Although prototypic steroidal downregulators such as 6a designed for intramuscular administration showed insufficient cellular potency, a medicinal chemistry program derived from a novel androgen receptor ligand 8a led to 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine (10b), for which high plasma levels following oral administration in a preclinical model compensate for moderate cellular potency.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Próstata
/
Piridazinas
/
Receptores Androgênicos
Limite:
Humans
/
Male
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article