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.
Keywords: 6-Oxa-estra-1,3,5(10),8(9)-tetraenes; Cholesterol-lowering and antioxidant properties; Decreased uterotrophic activity; Hormone replacement therapy; Osteoprotective; Stereoselectivity of hydrogenation reaction.
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