Synthesis and biological activity of some 8α-analogs of steroidal estrogens

被引:0
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作者
S. N. Morozkina
Sh. N. Abusalimov
S. I. Selivanov
A. G. Shavva
机构
[1] St. Petersburg State University,
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关键词
Raney Nickel; Steroidal Estrogen; Spectral Matrix; Sodium Dichromate; Hypocholesterolemic Activity;
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摘要
8α-Analogs of steroidal estrogens containing a methyl group on C1 or an oxo group on C6 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-8α-estrone as an example, such compounds in solution can exist as two conformers, whereas the oxo group on C6 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-8α-analogs showed osteoprotective activity, so that introduction of an oxo group into the 6-position is promising from the viewpoint of hormone replacement therapy.
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页码:603 / 609
页数:6
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