Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists

Several tetrahydrofluorenones with a triazole fused across C7–C8 showed high levels of ERβ-selectivity and were found to be potent ERβ-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERβ.

Graphical abstractSeveral tetrahydrofluorenones with a triazole fused across C7–C8 showed high levels of ERβ-selectivity and were found to be potent ERβ-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERβ.Figure optionsDownload full-size imageDownload as PowerPoint slide