Structure-based design, synthesis and in vitro characterization of potent 17β-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone

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

“…This approach led to compounds with comparably weak inhibitory activity on 17␤-HSD1 (IC 50 > 1 M). Computational studies suggested these substituents to target a lipophilic subpocket close to the C-terminal helix [88]. The 2-phenethyl-d-homo-estrone as the most active compound showed an IC 50 of 15 nM (inhibition of the reduction of 15 nM E1 in E. coli homogenate over-expressing His-tagged 17␤-HSD1).…”

A useful cell system for studying the regulation of 17HSD/KSR type 2 activity and expression in ovarian epithelial cancer

“…They should include the use of specific enzyme inhibitors such as the 17HSD/KSR type 1 inhibitor recently reported [54].…”

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.…”