Synthesis and study of B-nor-8-isoanalogs of steroid estrogens
Shavva, A.G.; Selivanov, S.I.; Starova, G.L.; Boronoeva, T.R.; Ishchenko, I.V.; Gluzdikov, I.A.; Sharetskiĭ, A.N.; Isaeva, V.G.; Surinov, B.P.
Bioorganicheskaia Khimiia 28(3): 242-250
2002
ISSN/ISBN: 0132-3423 PMID: 12077850 Document Number: 549197
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.