title: [Synthesis and study of B-nor-8-isoanalogs of steroid estrogens].
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.
authors.affiliation: Chemical Faculty, St. Petersburg State University, Universitetskii pr. 26, Staryi Petergof, St. Petersburg, 198504 Russia. nmr@paloma.spbu.ru
authors.forename: A G
authors.initials: AG
authors.lastname: Shavva
authors.forename: S I
authors.initials: SI
authors.lastname: Selivanov
authors.forename: G L
authors.initials: GL
authors.lastname: Starova
authors.forename: T R
authors.initials: TR
authors.lastname: Boronoeva
authors.forename: I V
authors.initials: IV
authors.lastname: Ishchenko
authors.forename: I A
authors.initials: IA
authors.lastname: Gluzdikov
authors.forename: A N
authors.initials: AN
authors.lastname: Sharetskiĭ
authors.forename: V G
authors.initials: VG
authors.lastname: Isaeva
authors.forename: B P
authors.initials: BP
authors.lastname: Surinov
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D004958:Estradiol / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D004967:Estrogens / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004970:Estrone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D007073:Immunoglobulin E / Q000096:biosynthesis; D007166:Immunosuppressive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D051379:Mice; D008810:Mice, Inbred C57BL; D008808:Mice, Inbred CBA; D008958:Models, Molecular; D015394:Molecular Structure; D009929:Organ Size; D010052:Ovariectomy; D051381:Rats; D017208:Rats, Wistar; D011960:Receptors, Estrogen / Q000737:chemistry; D014599:Uterus / Q000187:drug effects
chemical_list: C460859:16,16-dimethylhomo-B-nor-8-isoestrone; D004967:Estrogens; D007166:Immunosuppressive Agents; D008024:Ligands; D011960:Receptors, Estrogen; D004970:Estrone; D007073:Immunoglobulin E; D004958:Estradiol