Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives

Bioorg Med Chem Lett. 2000 Jan 17;10(2):147-51. doi: 10.1016/s0960-894x(99)00648-4.


A diastereomerically pure series of 7alpha-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor alpha and the more recently discovered estrogen receptor beta. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain.

MeSH terms

  • Binding, Competitive
  • Estradiol / analogs & derivatives*
  • Estradiol / metabolism
  • Estradiol / pharmacology
  • Estrogen Receptor Modulators / chemical synthesis*
  • Estrogen Receptor Modulators / pharmacology
  • Receptors, Estrogen / drug effects
  • Sulfhydryl Compounds / chemical synthesis*
  • Tamoxifen / analogs & derivatives


  • Estrogen Receptor Modulators
  • Receptors, Estrogen
  • Sulfhydryl Compounds
  • Tamoxifen
  • Estradiol