A novel estrogen receptor ligand template

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1919-22. doi: 10.1016/s0960-894x(03)00307-x.

Abstract

Three synthetic routes towards a novel estrogen receptor ligand template based on a rigid bicyclo-[3.3.1]-nonene core have been investigated. The prototype compound exhibits potent binding at the ERbeta receptor and promising estrogen receptor subtype selectivity.

Publication types

  • Comparative Study

MeSH terms

  • Alkenes / chemical synthesis
  • Alkenes / metabolism*
  • Alkenes / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
  • Bridged Bicyclo Compounds, Heterocyclic / metabolism*
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology
  • Cell Line, Tumor
  • Estradiol / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Ligands
  • Membrane Proteins / agonists
  • Membrane Proteins / metabolism
  • Presenilin-2
  • Raloxifene Hydrochloride / pharmacology
  • Receptors, Estrogen / antagonists & inhibitors
  • Receptors, Estrogen / metabolism*

Substances

  • Alkenes
  • Bridged Bicyclo Compounds, Heterocyclic
  • Ligands
  • Membrane Proteins
  • PSEN2 protein, human
  • Presenilin-2
  • Receptors, Estrogen
  • Raloxifene Hydrochloride
  • Estradiol