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The Synthesis and Properties of B-Nor-8-Isoanalogues of Steroid Estrogens

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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.

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Authors and Affiliations

  1. Chemical Faculty, St. Petersburg State University, Universitetskii pr. 26, Staryi Petergof, St. Petersburg, 198504, Russia

    A. G. Shavva, S. I. Selivanov, G. L. Starova, T. R. Boronoeva, I. V. Ishchenko, I. A. Gluzdikov, A. N. Sharetskii, V. G. Isaeva & B. P. Surinov

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  1. A. G. Shavva
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  2. S. I. Selivanov
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  3. G. L. Starova
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  4. T. R. Boronoeva
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  5. I. V. Ishchenko
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  6. I. A. Gluzdikov
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  7. A. N. Sharetskii
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  8. V. G. Isaeva
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  9. B. P. Surinov
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Shavva, A.G., Selivanov, S.I., Starova, G.L. et al. The Synthesis and Properties of B-Nor-8-Isoanalogues of Steroid Estrogens. Russian Journal of Bioorganic Chemistry 28, 215–223 (2002). https://doi.org/10.1023/A:1015708404708

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