[Acylhydrazones of 20-keto steroids and their transformations: I. Synthesis and properties of 1'-acyl-substituted 3'-methylandrosteno[16,17-d]pyrazolines].

Acetates of 3beta-hydroxy-3'-methyl-1'(N)-acylandrost-5-eno[16,17-d]pyrazolines bearing monothiooxamide acyl groups were synthesized during the study of approaches to the synthesis of 3'-methylandrosteno[16,17-d]azoles, promising biologically active analogues of 20-keto pregnenanes, and their properties were investigated. The cyclization of delta16-20-thiooxamidohydrazones to the corresponding heterocycles was shown to proceed under rigorous conditions and to depend partially on the nature of the oxamide grouping.

[A new class of cardiotonic steroids]. / Novyi klass kardiotonicheskikh steroidov.

A series of 23-oxosteroid derivatives have been synthesized and tested for their inhibiting Na+, K(+)-dependent ATPase from rat brain in the 1 x 10(-6)-1 x 10(-4) M concentrations. Natural 23-oxogenins from sea star Asterias amurensis and synthetic monoesters showed the inhibiting activity upto 50-55%. These compounds caused heart contraction in frogs at the level of the known cardiotonic strophanthin G, and inotropic activity on isolated heart of mollusk Spisula sachalinensis.

[Purification of a special estrogen-binding protein from the liver of rats by affinity chromatography on estradiol sepharose]. / Ochistka osobogo éstrogensviazyvaiushchego belka pecheni krys affinnoi khromatografiei na éstradiol-sefaroze.

A procedure has been developed for purification of a special rat liver estrogen-binding protein. It includes protein precipitation by ammonium sulfate, gel filtration, ion exchange chromatography, and affinity chromatography on estradiol sepharose. The protein is purified 2260-fold with a 27% yield. Upon electrophoresis in 10% PAG in the presence of sodium dodecylsulfate the protein gives one polypeptide strip with a molecular weight of 31.200 +/- 400 dalton.

[Molecular polarity dependence of the transformed steroid effect on Na,K-ATPase]. / Zavisimost' vliianiia transformirovannykh steroidov na Na,K-ATPazy ot bifil'nosti ikh molekul.

The transformed steroids containing an additional cycle E (delta-lactone or 16.23-pyranone) or 23-carbethoxy side chain (1.10(-5) M) inhibit Na,K-ATPase from pig kidney medulla. The steroid structure has a noticeable effect on ATPase inhibiton varying from 9 to 35%. The data obtained suggest that the position, stereochemistry and the uneven distribution of polar substituents in the steroid molecule are essential for ATPase inhibition by steroid aglycons.