Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.

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Schopfer U, Schoeffter P, Bischoff SF, Nozulak J, Feuerbach D, Floersheim P

Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.

J Med Chem. 2002 Mar 28;45(7):1399-401.

PubMed ID
11906280 [ View in PubMed
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Abstract

In an effort to identify selective ligands for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assays in HeLa and SH-SY5Y cells, compounds were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of endometrial and breast cancer.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
2-(4-hydroxyphenyl)benzo[b]thiophen-6-olEstrogen receptor alphaIC 50 (nM)14107.422Details
2-(4-hydroxyphenyl)benzo[b]thiophen-6-olEstrogen receptor alphaEC 50 (nM)507.422Details
DiethylstilbestrolEstrogen receptor alphaIC 50 (nM)127.422Details
DiethylstilbestrolEstrogen receptor alphaEC 50 (nM)0.067.422Details
DiethylstilbestrolEstrogen receptor betaIC 50 (nM)97.422Details
DiethylstilbestrolEstrogen receptor betaEC 50 (nM)0.027.422Details
EstradiolEstrogen receptor alphaIC 50 (nM)247.422Details
EstradiolEstrogen receptor alphaEC 50 (nM)0.027.422Details
EstradiolEstrogen receptor betaIC 50 (nM)247.422Details
EstradiolEstrogen receptor betaEC 50 (nM)0.077.422Details
EstroneEstrogen receptor alphaIC 50 (nM)4807.422Details
EstroneEstrogen receptor alphaEC 50 (nM)0.77.422Details
EstroneEstrogen receptor betaIC 50 (nM)11357.422Details
EstroneEstrogen receptor betaEC 50 (nM)2.17.422Details
GenisteinEstrogen receptor alphaIC 50 (nM)39207.422Details
GenisteinEstrogen receptor alphaEC 50 (nM)487.422Details
GenisteinEstrogen receptor betaIC 50 (nM)2007.422Details
GenisteinEstrogen receptor betaEC 50 (nM)4.17.422Details
RaloxifeneEstrogen receptor alphaIC 50 (nM)227.422Details
RaloxifeneEstrogen receptor betaIC 50 (nM)2607.422Details