Simple bi- and tricyclic inhibitors of human steroid 5alpha-reductase.
Bioorg Med Chem Lett
; 10(17): 1909-11, 2000 Sep 04.
Article
em En
| MEDLINE
| ID: mdl-10987415
ABSTRACT
A number of tricyclic thiolactams, bicyclic lactams, and bicyclic thiolactams have been prepared and evaluated in vitro as inhibitors of types 1 and 2 steroid 5alpha-reductase. The tricycles with an 8-chloro substituent in the C-ring are nM (IC50) inhibitors of type 1 steroid 5alpha-reductase (SR). In all the cases studied, lactams are more potent than the corresponding thiolactams. Activity against type 2 SR is greatly enhanced by a styryl (or azo) substituent on the aryl ring of the tri- and bicycles and also a related tricyclic aryl acid.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores Enzimáticos
/
Inibidores de 5-alfa Redutase
/
Lactamas
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2000
Tipo de documento:
Article
País de afiliação:
Nova Zelândia