Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Article Details
- CitationCopy to clipboard
Miller CP, Jirkovsky I, Tran BD, Harris HA, Moran RA, Komm BS
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Bioorg Med Chem Lett. 2000 Jan 17;10(2):147-51.
- PubMed ID
- 10673099 [ View in PubMed]
- Abstract
A diastereomerically pure series of 7alpha-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor alpha and the more recently discovered estrogen receptor beta. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Estradiol Estrogen receptor alpha EC 50 (nM) 0.007 N/A N/A Details Estradiol Estrogen receptor alpha IC 50 (nM) 3 N/A N/A Details Estradiol Estrogen receptor beta IC 50 (nM) 4 N/A N/A Details Fulvestrant Estrogen receptor alpha IC 50 (nM) 0.47 N/A N/A Details Fulvestrant Estrogen receptor alpha IC 50 (nM) 6 N/A N/A Details