Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.

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Tan Q, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3753-5.

PubMed ID
15203156 [ View in PubMed
]
Abstract

Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model.

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