Abstract
Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERbeta subtype selective ligands is described. Analogs possessing subnanomolar ERbeta binding, greater than 100-fold ERbeta-selectivity, and oral bioavailability are reported.
MeSH terms
-
Animals
-
Area Under Curve
-
Biological Availability
-
Cyclization
-
Estrogen Receptor beta / drug effects*
-
Estrogen Receptor beta / metabolism
-
Fluorenes / blood
-
Fluorenes / chemistry*
-
Fluorenes / metabolism
-
Pyrazoles / chemistry*
-
Rats
Substances
-
Estrogen Receptor beta
-
Fluorenes
-
Pyrazoles