Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
J Med Chem
; 49(26): 7596-9, 2006 Dec 28.
Article
em En
| MEDLINE
| ID: mdl-17181141
ABSTRACT
A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited >50-fold selectivity for muscle over prostate.
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Base de dados:
MEDLINE
Assunto principal:
Hidrocarbonetos Aromáticos com Pontes
/
Atrofia Muscular
/
Receptores Androgênicos
/
Músculo Esquelético
/
Hidantoínas
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article