Synthesis and receptor-binding examination of 16-hydroxymethyl-3,17-estradiol stereoisomers

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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-3,17β-diol. The affinities of the tested compounds for the androgen and progesterone receptors are very low (Ki> 100 μm and 1 μM, respectively). The prepared 16-hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers are therefore estrogen receptor-selective molecules.

Original languageEnglish
Pages (from-to)371-377
Number of pages7
JournalSteroids
Volume67
Issue number5
DOIs
Publication statusPublished - Mar 21 2002

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Keywords

  • 16-Hydroxymethylestra-1,3,5(10)-triene-3,17-diol isomers
  • Estrogen receptor binding

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology
  • Pharmacology
  • Clinical Biochemistry
  • Organic Chemistry

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