Estrogen receptor β-subtype selective tetrahydrofluorenones: Use of a fused pyrazole as a phenol bioisostere
2006
Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERβ subtype selective ligands is described. Analogs possessing subnanomolar ERβ binding, greater than 100-fold ERβ-selectivity, and oral bioavailability are reported.
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