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.
MeSH terms
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Animals
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Crystallography, X-Ray
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Estradiol / analogs & derivatives
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Estradiol / chemistry
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Estradiol / pharmacology
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Estrogens / chemical synthesis*
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Estrogens / chemistry
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Estrogens / pharmacology
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Estrone / analogs & derivatives*
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Estrone / chemical synthesis*
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Estrone / chemistry
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Estrone / pharmacology
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Female
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Immunoglobulin E / biosynthesis
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Immunosuppressive Agents / chemical synthesis
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / pharmacology
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Ligands
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Mice
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Mice, Inbred C57BL
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Mice, Inbred CBA
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Models, Molecular
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Molecular Structure
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Organ Size
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Ovariectomy
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Rats
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Rats, Wistar
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Receptors, Estrogen / chemistry
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Uterus / drug effects
Substances
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16,16-dimethylhomo-B-nor-8-isoestrone
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Estrogens
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Immunosuppressive Agents
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Ligands
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Receptors, Estrogen
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Estrone
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Immunoglobulin E
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Estradiol