[Synthesis and study of B-nor-8-isoanalogs of steroid estrogens]

Bioorg Khim. 2002 May-Jun;28(3):242-50.
[Article in Russian]

Abstract

The study of the binding of estradiol B-nor-8-isonalogues to estrogen receptors from the rat uterus helped create the proposed model of the corresponding ligand-receptor complexes. The use of this model ensured the choice of such micromodifications in this steroid group that sharply decreased their hormonal activity. By the example of 16,16-dimethyl-D-homo-B-nor-8-isoestrone, we demonstrated the possibility of the synthesis of the estrogen analogues devoid of uterotropic activity but retaining immunosuppressive activity.

Publication types

  • English Abstract

MeSH terms

  • Animals
  • Crystallography, X-Ray
  • Estradiol / analogs & derivatives
  • Estradiol / chemistry
  • Estradiol / pharmacology
  • Estrogens / chemical synthesis*
  • Estrogens / chemistry
  • Estrogens / pharmacology
  • Estrone / analogs & derivatives*
  • Estrone / chemical synthesis*
  • Estrone / chemistry
  • Estrone / pharmacology
  • Female
  • Immunoglobulin E / biosynthesis
  • Immunosuppressive Agents / chemical synthesis
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology
  • Ligands
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred CBA
  • Models, Molecular
  • Molecular Structure
  • Organ Size
  • Ovariectomy
  • Rats
  • Rats, Wistar
  • Receptors, Estrogen / chemistry
  • Uterus / drug effects

Substances

  • 16,16-dimethylhomo-B-nor-8-isoestrone
  • Estrogens
  • Immunosuppressive Agents
  • Ligands
  • Receptors, Estrogen
  • Estrone
  • Immunoglobulin E
  • Estradiol