Tetrahydroquinoline-based Selective Estrogen Receptor Modulators (SERMs)

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1907-10. doi: 10.1016/s0960-894x(03)00306-8.

Abstract

A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay.

MeSH terms

  • Cell Division / drug effects
  • Cell Line, Tumor
  • Humans
  • Hydroxyquinolines / chemical synthesis
  • Hydroxyquinolines / chemistry*
  • Hydroxyquinolines / pharmacology*
  • Inhibitory Concentration 50
  • Ligands
  • Receptors, Estrogen / agonists
  • Receptors, Estrogen / antagonists & inhibitors
  • Receptors, Estrogen / metabolism
  • Selective Estrogen Receptor Modulators / chemical synthesis
  • Selective Estrogen Receptor Modulators / chemistry*
  • Selective Estrogen Receptor Modulators / pharmacology*
  • Structure-Activity Relationship

Substances

  • Hydroxyquinolines
  • Ligands
  • Receptors, Estrogen
  • Selective Estrogen Receptor Modulators