New selective nonsteroidal aromatase inhibitors:: Synthesis and inhibitory activity of 2, 3 or 5-(α-azolylbenzyl)-1H-indoles

被引：57

作者：

Le Borgne, M

Marchand, P

Delevoye-Seiller, B

Robert, JM

Le Baut, G

Hartmann, RW

Palzer, M

机构：

[1] Fac Pharm, Chim Therapeut Lab, F-44035 Nantes, France

[2] Fac Pharm, Chim Organ Lab, F-44035 Nantes, France

[3] Univ Saarland, Fachrichtung Pharmazeut & Med Chem 12 1, D-66041 Saarbrucken, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(98)00737-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Six azolyl substituted indoles were synthesized and tested for their activity to inhibit two P450 enzymes: P450 arom and P450 17 alpha. It was observed that the introduction of alpha-imidazolylbenzyl chain at carbon 3 or 5 on indole nucleus led to very active molecules. Compounds 22, 23 and especially 33 demonstrate very high potential against P450 arom. Under our assay conditions of high substrate concentration the IC50 are 0.057, 0.0785 and 0.041 mu M,respectively. These compounds are moderate inhibitors against P450 17 alpha. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：333 / 336

页数：4

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