The discovery of tetrahydrofluorenones as a new class of estrogen receptor β-subtype selective ligands

Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERβ subtype selective ligands are described. Several analogs possessing ERβ binding affinities comparable to 17β-estradiol but with greater than 75-fold selectivity over ERα are reported.

Graphical abstractSynthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERβ subtype-selective ligands are described.Figure optionsDownload full-size imageDownload as PowerPoint slide