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The size and/or configuration of the cycloalkane D′ ring in pentacyclic progesterone derivatives are crucial for their high-affinity binding to a protein in addition to progesterone receptor in rat
[(3)H]labeled progesterone and a number of its 16alpha, 17alpha-cycloalkano derivatives with an additional three to six-membered D' ring were investigated for mutual competition and equilibriumExpand
[Species and tissue distribution specificity of proteins binding 16alpha,17alpha-cycloalkane derivatives of progesterone].
The binding of [3H]progesterone and [3H] 16 alpha,17 alpha-cycloalkanoprogesterones to proteins from rat, rabbit, and human uteri and other organs was studied. We found that 16 alpha,17Expand
Synthesis of [3H]-cycloalkanoprogesterones (pregna-d'-pentaranes) and study of their interaction with a progesterone receptor
In order to search target organs and to study the mechanism of the action of steroids with separated biological functions, tritium-labeled pregna-d'-pentaranes were synthesized by an originalExpand
Interactions of 16alpha,17alpha-cyclohexane derivatives of progesterone with the progesterone receptor from rat uterus.
Pregna-D'-pentaranes, 16alpha,17alpha-cyclohexanoprogesterone and 6alpha-methyl-16alpha,17alpha-cyclohexanoprogestero ne, were found to specifically interact with the progesterone receptor of solubleExpand
[Pentacyclic steroid analogs: interaction of 16 alpha,17 alpha-cyclopentanoprogesterone with rat uterus proteins].
Using 3H-labeled derivatives, kinetic parameters of specific binding of progesterone (I) and 16 alpha, 17 alpha-cyclopentanoprogesterone (II) to proteins of the uterus soluble fraction in rats wereExpand
Synthesis of (5Z,8Z,11Z,14Z)-18- and 19-azidoeicosa-5,8,11,14-tetraenoic acids and their [5,6,8,9,11,12,14,15-3H8]-analogues through a common synthetic route.
Total synthesis of (5Z,8Z,11Z,14Z)-18- and 19-azidoeicosa-5,8,11,14-tetraenoic acids and their [5,6,8,9,11,12,14,15-3H8]-analogues via the corresponding p-toluenesulphonates is reported. ThisExpand
A convergent synthesis of (17R,5Z,8Z,11Z,14Z)-17-hydroxyeicosa-5,8,11,14-tetraenoic acid analogues and their tritiated derivatives
Abstract 17(R)-OH-AA and 14,15-dehydro-17(R)-OH-AA were synthesized from a common tetraacetylenic precursor and their azide derivatives were obtained in moderate yields via the correspondingExpand
The Synthesis of Tritium-Labeled 16α,17α-Cyclohex-3′-eno-progesterone as Probe for the Study of Steroid–Receptor Binding
Abstract Tritium-labeled 16α,17α-cyclohex-3′-en-pregn-4-en-3,20-dione (16α, 17α-cyclohex-3′-eno-progesterone) with specific activity of 44 Ci/mmol, required in studying of binding with progesteroneExpand
16α,17α-Cycloalkane Derivatives of Progesterone Intensively Bind to a Rat Serum Protein
The interaction of 6α-methyl-[1,2-3H]16α,17α-cyclohexanoprogesterone with rat serum proteins has been studied. Specific binding of this ligand characterized by Kd = 0.36 ± 0.10 μM and concentrationExpand