Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
ACS Med Chem Lett
; 2(2): 148-53, 2011 Feb 10.
Article
em En
| MEDLINE
| ID: mdl-24900294
ABSTRACT
We report the synthesis and characterization of novel 3-aryl indoles as potent and efficacious progesterone receptor (PR) antagonists with potential for the treatment of uterine fibroids. These compounds demonstrated excellent selectivity over other steroid nuclear hormone receptors such as the mineralocorticoid receptor (MR). They were prepared from 2-bromo-6-nitro indole in four to six steps using a Suzuki cross-coupling as the key step. Compound 8f was orally active in the complement 3 model of progesterone antagonism in the rat uterus and demonstrated partial antagonism in the McPhail model of progesterone activity.
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Bases de dados:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos