Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2729-33. doi: 10.1016/j.bmcl.2004.03.077.

Abstract

Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.

MeSH terms

  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Estrogen Receptor alpha / chemistry
  • Estrogen Receptor beta / chemistry
  • Female
  • Humans
  • Inhibitory Concentration 50
  • Ligands
  • Protein Binding
  • Selective Estrogen Receptor Modulators / chemical synthesis*
  • Selective Estrogen Receptor Modulators / pharmacology
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines / chemical synthesis
  • Tetrahydroisoquinolines / pharmacology*

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Ligands
  • Selective Estrogen Receptor Modulators
  • Tetrahydroisoquinolines