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

被引：41

作者：

Pouget, C ^{[1
]}

Fagnere, C ^{[1
]}

Basly, JP ^{[1
]}

Habrioux, G ^{[1
]}

Chulia, AJ ^{[1
]}

机构：

[1] Fac Pharm, UPRES EA Biomol & Cibles Cellulaires Tumorales 10, F-87025 Limoges, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(02)00072-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two (L)-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. (C), 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1059 / 1061

页数：3

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