New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.

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Pouget C, Fagnere C, Basly JP, Habrioux G, Chulia AJ

New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1059-61.

PubMed ID
11909717 [ View in PubMed
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Abstract

Two (E)-pyridinyl-substituted flavanone derivatives were synthesized and UV irradiation of these compounds afforded a Z-enriched mixture. These products were tested for their ability to inhibit the cytochrome P450 aromatase. It was observed that the introduction of a pyridinylmethylene group at carbon 3 on flavanone nucleus led to a significant increase of aromatase inhibitory effect. Moreover, configuration had a substantial influence on the aromatase inhibitory activity since (E)-isomers were found to be more active than (Z)-isomers.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AminoglutethimideCytochrome P450 19A1IC 50 (nM)5200N/AN/ADetails