Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2027890 | Steroids | 2014 | 5 Pages |
•New 7α-methyl-6-oxa-estrogens with cis-/trans-C/D rings junction.•Strong osteoprotective, cholesterol-lowering, antioxidant and less hormonal actions.•That is the advantage in comparison with clinically used 17α-ethynylestradiol.•Synthesized compounds are the candidates for clinical investigations.
To investigate the relationship between structure and biological activity of analogues of steroid estrogens we have developed the synthesis of 7α-methyl-6-oxa-estra-1,3,5(10),8(9)-tetraenes with cis- and trans-junction of C and D rings. We found that such compounds have stronger osteoprotective, cholesterol-lowering and antioxidant properties in comparison with uterotrophic activity; that is the advantage in comparison with clinically used 17α-ethynylestradiol.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide