Abstract
The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity.
MeSH terms
-
Antineoplastic Agents / metabolism
-
Antineoplastic Agents / pharmacology
-
Crystallography, X-Ray
-
Drug Design*
-
Estrogen Receptor alpha / metabolism*
-
Estrogen Receptor beta / metabolism*
-
Genistein / metabolism
-
Genistein / pharmacology
-
Humans
-
Indans / chemical synthesis*
-
Indans / chemistry
-
Indans / metabolism*
-
Ligands
-
Models, Molecular
-
Radioligand Assay
-
Structure-Activity Relationship
-
Substrate Specificity
Substances
-
1,2-indanedione
-
Antineoplastic Agents
-
Estrogen Receptor alpha
-
Estrogen Receptor beta
-
Indans
-
Ligands
-
Genistein