Diaryl-substituted salicyl- and anthranyl-ketoximes as potential estrogen receptor ligands

Farmaco. 2004 Aug;59(8):601-7. doi: 10.1016/j.farmac.2004.01.007.

Abstract

3,4-diphenylsalicylaldoxime and 3,4-diphenylanthranylaldoxime derivatives, containing small groups (methyl or ethyl) on the imine carbon atom, were synthesized and submitted to biological assays. Binding tests performed on uterine cytosol estrogen receptor (ER) preparation and on purified full-length human ERalpha and ERbeta, showed that the newly synthesised compounds exhibit considerably lower binding affinities with respect to reference non-substituted 3,4-salicylaldoxime.

MeSH terms

  • Binding, Competitive / drug effects
  • Estrogen Receptor alpha / agonists
  • Estrogen Receptor alpha / antagonists & inhibitors
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / agonists
  • Estrogen Receptor beta / antagonists & inhibitors
  • Estrogen Receptor beta / metabolism
  • Humans
  • Ligands
  • Molecular Structure
  • Oximes / chemical synthesis*
  • Oximes / chemistry
  • Oximes / pharmacology*
  • Receptors, Estrogen / agonists
  • Receptors, Estrogen / antagonists & inhibitors*
  • Receptors, Estrogen / metabolism
  • Structure-Activity Relationship

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Ligands
  • Oximes
  • Receptors, Estrogen