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Preparation and Bioavailability Evaluation of Micronized Steroidal Mecigestone Drug Substance
Microcrystals of 6α-methyl-16α,17α-cyclohexapregn-4-ene-3,20-dione (mecigestone) that differed from the starting drug substance by decreased sizes and altered morphologies were produced using a NanoExpand
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
Relationship between structure and mode of action of 16 alpha, 17 alpha-cycloalkanoprogesterones (pregna-D'-pentaranes).
A new class of modified progesterones with an additional 16 alpha, 17 alpha-carbocycle (pregna-D'-pentaranes) is obtained. These compounds were found to exhibit a high progestational activity in theExpand
Synthesis of tritium‐labelled biologically active analogues of progesterone by selective hydrogenation of 16α,17α‐cyclohex‐3′‐en‐pregna‐1,4‐dien‐3,20‐dione
The procedure of selective hydrogenation with gaseous tritium of 16α,17α-cyclohex-3'-en-pregna-1,4-dien-3,20-dione (StO) has been elaborated, and isotopically labelledExpand
Steroids fused to heterocycles at positions 16, 17 of the D-ring
Syntheses of modified steroids annulated at the 16-, 17-positions with five- and six-membered heterocycles are reviewed. The biological activity profiles of these compounds as important secondaryExpand
[Molecular docking and 3D-QSAR on 16alpha,17alpha-cycloalkanoprogesterone analogues as progesterone receptor ligands].
A series of 42 steroid ligands was used to predict a binding affinity to progesterone receptor. The molecules were the derivatives of 16alpha,17alpha-cycloalkanoprogesterones. Different methods ofExpand
3- and 19-Oximes of 16α,17α-cyclohexanoprogesterone derivatives: Synthesis and interactions with progesterone receptor and other proteins
Series of 3- and 19-oximes of 16alpha,17alpha-cyclohexanoprogesterone derivatives (pregna-d'-pentaranes) have been synthesized with the aim of probing the surfaces of progesterone receptor's and twoExpand
New estrogen receptor antagonists. 3,20-Dihydroxy-19-norpregna-1,3,5(10)-trienes: Synthesis, molecular modeling, and biological evaluation.
New estrogen receptor α (ERα) antagonists - 3,20-dihydroxy-19-norpregna-1,3,5(10)-trienes containing an additional carbocyclic ring D' at the 16α,17α positions - were synthesized. The effects of theExpand
Approaches to the design of selective ligands for membrane progesterone receptor alpha
A number of progesterone derivatives were assayed in terms of their affinity for recombinant human membrane progesterone receptor alpha (mPRα) in comparison with nuclear progesterone receptor (nPR).Expand
Selection of progesterone derivatives specific to membrane progesterone receptors
The search of selective agonists and antagonists of membrane progesterone receptors (mPRs) is a starting point for the study of progesterone signal transduction mechanisms mediated by mPRs, distinctExpand