Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes

► Salicylaldoxime pseudocycle proves to be an efficient bioisosteric replacement of phenol. ► Improved selective binding to ER-beta is obtained by structural optimization of salicylaldoximes. ► Chloro/fluoro-substituted Salaldox B members show a binding affinity for ER-beta similar to that of estradiol. ► The best ER-beta ligands confirm their beta-selective full agonist properties. ► Docking analysis indicates a peculiar H-bond formation with Thr299 of ER-beta.