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

Bioorganic & Medicinal Chemistry Letters
Christelle PougetAlbert-José Chulia

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.

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Citations

Aug 12, 2008·Anti-cancer Agents in Medicinal Chemistry·Marcy J BalunasA Douglas Kinghorn
Apr 15, 2004·Biochemical and Biophysical Research Communications·Cédric Gaudineau, Karine Auclair
Sep 27, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Liang-Peng SunHu-Ri Piao
Sep 2, 2018·Medicinal Research Reviews·Alexander J Nielsen, James McNulty
Oct 3, 2008·Chemistry, an Asian Journal·Midori A AraiMasami Ishibashi
May 18, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jacek KędziaTomasz Janecki

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