Androstene-3,5-dienes as ER-beta selective SERMs.

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Blizzard TA, Gude C, Morgan JD 2nd, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Rohrer SP, Hammond ML

Androstene-3,5-dienes as ER-beta selective SERMs.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.

PubMed ID
17890084 [ View in PubMed
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Abstract

A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist and was more selective for ER-beta over the androgen receptor (AR).

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