Synthesis and investigation of biological properties of modified 6-oxa-estra-1,3,5(10),8(9)-tetraenes

• 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.

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