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

Bioorg Med Chem Lett

UPRES EA 1085, Biomolécules et cibles cellulaires tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, 87025 Limoges cedex, France.

Published: April 2002

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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http://dx.doi.org/10.1016/s0960-894x(02)00072-0DOI Listing

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