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The aim of this study was to ascertain the inhibitory effect of several progesterone derivatives for 5α-reductase types 1 and 2 isozymes and to determine the binding to the androgen receptor.The 3,20-dioxopregna-4-ene-17α-yl acetate 4 containing an acetoxy group in C-17 and steroid 17α-hydroxypregn-4-ene-3,20-dione 5 having a hydroxyl group in the same position inhibited both isozymes. On the other...
A mild and efficient Δ 1 -dehydrogenation of Δ 4 -3-keto-steroids with DDQ in the presence of tertbutyldimethylchlorosilane at room temperature was developed.
Synthesis, aggregation behavior and in vitro cholesterol solubilization studies of 16-epi-pythocholic acid (3α,12α,16β-trihydroxy-5β-cholan-24-oic acid, EPCA) are reported. The synthesis of this unnatural epimer of pythocholic acid (3α,12α,16α-trihydroxy-5β-cholan-24-oic acid, PCA) involves a series of simple and selective chemical transformations with an overall yield of 21% starting from readily...
Steroid hormones participate in organ development, reproduction, body homeostasis, and stress responses. The steroid machinery is expressed in a development- and tissue-specific manner, with the expression of these factors being tightly regulated by an array of transcription factors (TFs). Epigenetics provides an additional layer of gene regulation through DNA methylation and histone tail modifications...
17α-substituted ethynylestradiols, derived from estrone, were converted to their corresponding 17α-(bromo- or iodo-propargyl)estrone intermediates. Nucleophilic substitution onto these moieties with malonate diester followed by hydrolysis and complexation with cis-Pt(Me 2 en)I 2 (Me 2 en=N,N-dimethylethylenediamine) gave cis-Pt(Me 2 en)(2-(3-(17β-estradiol-17α-yl)-prop-2-ynyl)malonato)...
In this review we describe procedures, performance characteristics and limitations of methods available for the measurement of 25-hydroxyvitamin (25OHD) since the year 2000. The two main types of methods are competitive immunoassay and those based on chromatographic separation followed by non-immunological direct detection (HPLC, LC–MS/MS). Lack of a reference standard for 25OHD has, until recently,...
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