Preparation and pharmacological profile of 7-(α-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors

被引：39

作者：

Marchand, P

Le Borgne, M

Palzer, M

Le Baut, G

Hartmann, RW

机构：

[1] UFR Sci Pharmaceut, Lab Chim Organ & Chim Therapeut, F-44035 Nantes, France

[2] Univ Saarland, D-66041 Saarbrucken, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(03)00182-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aromatase (P450 arom) is a target of pharmacological interest for the treatment of breast cancer. New series of 7-(alpha-azolylbenzyl)-1H-indoles and indolines were synthesized as non-steroidal inhibitors of P450 arom. Selectivity was studied towards P450 17alpha enzyme. The most active compound, 1-ethyl-7-[(imidazol-1-yl)(4-chlorophenyl)methyl]-1H-indole 12c exhibited promising relative potency (rp) of 336 (rp, of aminoglutethimide = 1) and most of the described azoles were active and selective towards P450 arom. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：1553 / 1555

页数：3

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