Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta
Language English Country United States Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
20408532
DOI
10.1021/jm901898a
Knihovny.cz E-resources
- MeSH
- Transcriptional Activation MeSH
- Estrogen Receptor alpha agonists genetics MeSH
- Alkynes chemistry MeSH
- Estrogen Receptor beta agonists genetics MeSH
- Cell Line MeSH
- Cyclization MeSH
- Estradiol analogs & derivatives chemical synthesis pharmacology MeSH
- Fluorescence Polarization MeSH
- Binding, Competitive MeSH
- Humans MeSH
- Ligands MeSH
- Luciferases genetics MeSH
- Cell Line, Tumor MeSH
- Drug Partial Agonism MeSH
- Cell Proliferation drug effects MeSH
- Genes, Reporter MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Estrogen Receptor alpha MeSH
- Alkynes MeSH
- Estrogen Receptor beta MeSH
- Estradiol MeSH
- Ligands MeSH
- Luciferases MeSH
To identify novel estrogen receptor ligands a series of substituted 17alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPh(3))(3)Cl]. The compounds were subjected to competitive binding assays, cell-based luciferase reporter assays, and proliferation assays. These experiments confirmed their estrogenic character and revealed some interesting properties like mixed partial/full agonism for ERalpha/ERbeta and different selectivity as a result of differing potencies for either ER.
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