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
收藏
页码：1059 / 1061
页数：3
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