Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Bioorg Med Chem Lett
; 19(8): 2139-43, 2009 Apr 15.
Article
in En
| MEDLINE
| ID: mdl-19321341
ABSTRACT
A series of dihydro-9,10-ethano-anthracene-11-carboxamides as novel glucocorticoid receptor modulators is reported. SAR exploration identified compounds from this series displaying a promising dissociation profile in discriminating between transrepression and transactivation activities. 17a is a partial agonist of GR-mediated transactivation which elicits potent and efficacious transrepression in reporter gene assays. A hypothetical binding mode is provided which accounts for the induction of functional activity by a bridgehead methyl group.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, Glucocorticoid
/
Drug Discovery
/
Anthracenes
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2009
Document type:
Article
Affiliation country:
United States