Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.

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Blizzard TA, DiNinno F, Morgan JD 2nd, Chen HY, Wu JY, Gude C, Kim S, Chan W, Birzin ET, Tien Yang Y, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3861-4.

PubMed ID
15225685 [ View in PubMed
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Abstract

A series of benzoxathiin SERAMs with bicyclic amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Compound 4-DEstrogen receptor alphaIC 50 (nM)0.8N/AN/ADetails
EstradiolEstrogen receptor alphaIC 50 (nM)1.3N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)1.1N/AN/ADetails
RaloxifeneEstrogen receptor alphaIC 50 (nM)1.8N/AN/ADetails
RaloxifeneEstrogen receptor betaIC 50 (nM)12N/AN/ADetails