Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.
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SUBMITTER: Bertini S
PROVIDER: S-EPMC3088081 | biostudies-literature | 2011 Jun
REPOSITORIES: biostudies-literature
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Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.
Bertini Simone S De Cupertinis Andrea A Granchi Carlotta C Bargagli Barbara B Tuccinardi Tiziano T Martinelli Adriano A Macchia Marco M Gunther Jillian R JR Carlson Kathryn E KE Katzenellenbogen John A JA Minutolo Filippo F
European journal of medicinal chemistry 20110323 6
In a continuing effort to improve the subtype selectivity and agonist potency of estrogen receptor β (ERβ) ligands, we have designed and developed a thus far unexplored structural series obtained by molecular refinements of monoaryl-substituted salicylaldoximes (Salaldox B). The most interesting compounds in this series (2c, d) show remarkably high ERβ-binding affinities, with Ki values reaching the sub-nanomolar range (Ki=0.38 nM for 2c and 0.57 nM for 2d), and have very high levels of ERβ-subt ...[more]
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