Результаты исследований: Научные публикации в периодических изданиях › статья
Synthesis and biological activity of some 8 alpha-analogs of steroidal estrogens. / Morozkina, S.N.; Abusalimov, Sh.N.; Selivanov, S.I.; Shavva, A.G.
в: Russian Journal of Organic Chemistry, Том 49, № 4, 2013, стр. 603-609.Результаты исследований: Научные публикации в периодических изданиях › статья
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TY - JOUR
T1 - Synthesis and biological activity of some 8 alpha-analogs of steroidal estrogens
AU - Morozkina, S.N.
AU - Abusalimov, Sh.N.
AU - Selivanov, S.I.
AU - Shavva, A.G.
PY - 2013
Y1 - 2013
N2 - 8 alpha-Analogs of steroidal estrogens containing a methyl group on C-1 or an oxo group on C-6 were synthesized with a view to obtain compounds exhibiting selective biological activity, and their steric structure was studied. As shown with 1,3-O-dimethyl-8 alpha-estrone as an example, such compounds in solution can exist as two conformers, whereas the oxo group on C-6 almost does not affect conformation of the modified derivative as compared to the parent structure. Some newly synthesized compounds exhibited hypocholesterolemic activity in combination with reduced uterotropic effect, which is important for the design of drugs for the treatment of atherosclerosis. 6-Oxo-8 alpha-analogs showed osteoprotective activity, so that introduction of an oxo group into the 6-position is promising from the viewpoint of hormone replacement therapy.
AB - 8 alpha-Analogs of steroidal estrogens containing a methyl group on C-1 or an oxo group on C-6 were synthesized with a view to obtain compounds exhibiting selective biological activity, and their steric structure was studied. As shown with 1,3-O-dimethyl-8 alpha-estrone as an example, such compounds in solution can exist as two conformers, whereas the oxo group on C-6 almost does not affect conformation of the modified derivative as compared to the parent structure. Some newly synthesized compounds exhibited hypocholesterolemic activity in combination with reduced uterotropic effect, which is important for the design of drugs for the treatment of atherosclerosis. 6-Oxo-8 alpha-analogs showed osteoprotective activity, so that introduction of an oxo group into the 6-position is promising from the viewpoint of hormone replacement therapy.
U2 - 10.1134/S1070428013040180
DO - 10.1134/S1070428013040180
M3 - Article
VL - 49
SP - 603
EP - 609
JO - Russian Journal of Organic Chemistry
JF - Russian Journal of Organic Chemistry
SN - 1070-4280
IS - 4
ER -
ID: 7521958