Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Bioorg Med Chem Lett
; 17(18): 5025-31, 2007 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-17692519
ABSTRACT
A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To identify compounds with an improved side effect profile over marketed steroids the functional activity of compounds was evaluated in cell based assays for transactivation (aromatase) and transrepression (IL-6). Through this effort, 36 has been identified as a partial agonist with a dissociated profile in these cell based assays.
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Base de dados:
MEDLINE
Assunto principal:
Glucocorticoides
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article