Abstract
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
MeSH terms
-
Cell Line
-
Crystallography, X-Ray
-
Estrogen Receptor alpha / chemistry
-
Estrogen Receptor alpha / drug effects
-
Estrogen Receptor beta / chemistry
-
Estrogen Receptor beta / drug effects*
-
Fluorenes / chemical synthesis*
-
Fluorenes / classification
-
Fluorenes / pharmacology*
-
Humans
-
Ligands
-
Models, Molecular
-
Molecular Structure
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
4-bromo-9a-butyl-7-hydroxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one
-
Estrogen Receptor alpha
-
Estrogen Receptor beta
-
Fluorenes
-
Ligands