Article ID Journal Published Year Pages File Type
1373309 Bioorganic & Medicinal Chemistry Letters 2009 5 Pages PDF
Abstract

The effect of 32 flavonoids on androgen (AR) and glucocorticoid receptors (GR) was investigated using an MDA-kb2 human breast cancer cell line to predict potential AR and GR activities. Among them, 5-hydroxyflavone (7) had the highest AR antagonistic activity with an IC50 value of 0.3 μM, whereas 6-methoxyflavone (11) had the highest induced luciferase activity with an EC150 value of 0.7 μM. Genistein (2) and daizein (1) showed a sufficient increase of luciferase activities as their concentrations increased with EC150 values of 4.4 and 10.1 μM, respectively. These findings provide evidence of a fundamental property of their structure–activity relationship with AR and/or GR.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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