Novel estrone mimetics with high 17β-HSD1 inhibitory activity

17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: Protein structures, functions, and recent progress in inhibitor development

“…Heterocyclic substituted biphenylols and their aza-analogs bearing only one OH-group [103], were recently found to inhibit 17␤-HSD1 (Fig. 10).…”

“…A change in selectivity preference induced by minor structural modifications was also observed in the class of heterocyclic substituted biphenylols. The 17␤-HSD2 inhibitor 24 (IC 50 17␤-HSD2 470 nM vs. 17␤-HSD1 2380 nM) was transformed into a 17␤-HSD1 inhibitor by changing the position of the nitrogen [103].…”

Bicyclic Substituted Hydroxyphenylmethanone Type Inhibitors of 17 β‐Hydroxysteroid Dehydrogenase Type 1 (17 β‐HSD1): The Role of the Bicyclic Moiety

“…[44,45] The phenyl ring adjacent to the thiophene was found to mimic the steroidal A ring binding in the C-terminal region of the protein.…”

Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker

“…Both steroidal [18,19] and non-steroidal [20][21][22][23][24][25][26][27][28][29][30][31] 17β-HSD1 inhibitors have been described in the past. Recently we reported on bicyclic substituted hydroxyphenylmethanones [32] (general structure, fig.…”