Synthesis and receptor-binding examination of 16-hydroxymethyl-3,17-estradiol stereoisomers |
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Authors: | Tapolcsányi Pál Wölfling János Falkay George Márki Arpád Minorics Renáta Schneider Gyula |
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Affiliation: | Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary. |
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Abstract: | The four 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers were synthesized and tested in a radioligand-binding assay. The estrogen receptor recognizes these compounds, but their relative binding affinities are lower than 2.0% relative to that of the reference molecule estra-1,3,5(10)-triene-3,17beta-diol. The affinities of the tested compounds for the androgen and progesterone receptors are very low (K(i)> 100 microm and 1 microM, respectively). The prepared 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers are therefore estrogen receptor-selective molecules. |
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