Aza analogues of equol: novel ligands for estrogen receptor beta.

Article Details

Citation
Copy to clipboard

Chen W, Lin Z, Ning M, Yang C, Yan X, Xie Y, Shen X, Wang MW

Aza analogues of equol: novel ligands for estrogen receptor beta.

Bioorg Med Chem. 2007 Sep 1;15(17):5828-36. Epub 2007 Jun 6.

PubMed ID
17574424 [ View in PubMed
]
Abstract

3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERalpha and ERbeta. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: antagonists for ERalpha and agonists for ERbeta in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
GenisteinEstrogen receptor alphaEC 50 (nM)810N/AN/ADetails
GenisteinEstrogen receptor alphaIC 50 (nM)580N/AN/ADetails
GenisteinEstrogen receptor betaIC 50 (nM)6.8N/AN/ADetails
GenisteinEstrogen receptor betaEC 50 (nM)28N/AN/ADetails