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

被引:1
|
作者
Morozkina, S. N. [1 ]
Abusalimov, Sh. N. [1 ]
Selivanov, S. I. [1 ]
Shavva, A. G. [1 ]
机构
[1] St Petersburg State Univ, St Petersburg 198504, Russia
关键词
HORMONE-REPLACEMENT THERAPY; MILLION WOMEN; CARCINOGENESIS; IDENTIFICATION; SPECTROSCOPY; CANCER; RISK;
D O I
10.1134/S1070428013040180
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:603 / 609
页数:7
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