Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.

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Hamann LG, Meyer JH, Ruppar DA, Marschke KB, Lopez FJ, Allegretto EA, Karanewsky DS

Structure-activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor alpha/beta agonist scaffold.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1463-6.

PubMed ID
15713407 [ View in PubMed
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Abstract

An oxabicyclic template for estrogen receptor alpha and beta agonists has been identified which can be tuned to provide moderate levels of selectivity for either receptor sub-type. Structure-activity relationships within this phenol-substituted oxabicyclo[3.3.1]nonene series are described. Select compounds from the present series showed activity in vivo after oral dosing in rodent models of uterine proliferation.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor betaEC 50 (nM)9.7N/AN/ADetails