2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Bioorg Med Chem Lett
; 17(20): 5704-8, 2007 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-17822897
ABSTRACT
The 2-azadecalin ring system was evaluated as a scaffold for the preparation of glucocorticoid receptor (GR) antagonists. High affinity, selective GR antagonists were discovered based on a hypothetical binding mode related to the steroidal GR antagonist RU-43044. 2-Benzenesulfonyl substituted 8a-benzyl-hexahydro-2H-isoquinolin-6-ones exemplified by (R)-37 had low nanomolar affinity for GR with moderate functional activity (200 nM) in a reporter gene assay. These compounds were devoid of affinity for other steroidal receptors (ER, AR, MR, and PR). Analogues based on an alternative putative binding mode (CP-like) were found to be inactive.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Enxofre
/
Benzeno
/
Receptores de Glucocorticoides
/
Hidrogênio
/
Isoquinolinas
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article