Abstract: The aim of this work was to study the ability of some estrogen 8a-analogues, that have CH 3 -group in the C-3 position, exhibit osteoprotective and cholesterolemic effects. The properties of these analogues was comparisoned with effects of native estradiol and 17a-ethynylestradiol (EE). We showed that compounds 3 ((d,l)-17b-acethoxy-3-methoxy-8a-estra-1,3,5(10)-triene) and 4 ((d,l)-3-methoxy-8a-estra-1,3,5(10)-triene-17-one) had the same osteoprotective and cholesterolemic effects as EE. The utherotropic effects of compound 3 and EE were the same, while the utherotropic activity of 17-keto derivative (compound 4) was higher than effect of EE. The osteoprotective and cholesterolemic effects of compounds 5 and 6 (d- or l-17b-acethoxy-3-methoxy- 13-ethyl-8a-gone-1,3,5(10)-triene) were approximately the same, however the utherotropic action of these compounds was different: the compound 5 had significantly lower activity, but the compound 6 had the same effect in comparison with EE. Thus, all studied estrogen 8a-analogues may be used as basic constructions for structural modifications which is necessary as medications with while spectrum of biological properties.
Reference: Eschenko N.D., Putilina F.E., Galkina O.V., Vilkova V.A., Zacharova L.I., Fidarov A.F., Morozkina S.N., Shavva A.G., Study of osteoprotective and hypolipidemic effects of estrogen 8a a-analogues, Biomeditsinskaya khimiya, 2015, vol:
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