Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.

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

Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3865-8.

PubMed ID
15225686 [ View in PubMed
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Abstract

A series of benzoxathiin SERAMs with heteroatom-substituted 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