Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
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Kim S, Wu J, Chen HY, Birzin ET, Chan W, Yang YT, Colwell L, Li S, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Bioorg Med Chem Lett. 2004 Jun 7;14(11):2741-5.
- PubMed ID
- 15125925 [ View in PubMed]
- Abstract
A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Compound 4-D Estrogen receptor alpha IC 50 (nM) 0.8 N/A N/A Details Compound 4-D Estrogen receptor alpha IC 50 (nM) 3 N/A N/A Details Compound 4-D Estrogen receptor alpha IC 50 (nM) 23 N/A N/A Details Compound 4-D Estrogen receptor alpha IC 50 (nM) 9.6 N/A N/A Details Raloxifene Estrogen receptor alpha IC 50 (nM) 1.8 N/A N/A Details Raloxifene Estrogen receptor beta IC 50 (nM) 12 N/A N/A Details