Bridged androstenediol analogs as ER-beta selective SERMs.

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Blizzard TA, Gude C, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Holmes MA, Rohrer SP, Hammond ML

Bridged androstenediol analogs as ER-beta selective SERMs.

Bioorg Med Chem Lett. 2007 May 15;17(10):2944-8. Epub 2006 Dec 21.

PubMed ID
17448656 [ View in PubMed
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Abstract

A series of bridged androstenediol derivatives was prepared. The bridged compounds exhibited reduced ER-beta selectivity relative to uncyclized analogs.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)1.4N/AN/ADetails
EstradiolEstrogen receptor alphaEC 50 (nM)0.75N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)1.2N/AN/ADetails
EstradiolEstrogen receptor betaEC 50 (nM)2.1N/AN/ADetails
TestosteroneAndrogen receptorIC 50 (nM)2.7N/AN/ADetails
TestosteroneEstrogen receptor alphaIC 50 (nM)>10000N/AN/ADetails