Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase

被引：42

作者：

Menear, Keith A. ^{[1
]}

Adcock, Claire ^{[1
]}

Alonso, Francisco Cuenca ^{[1
]}

Blackburn, Kristel ^{[1
]}

Copsey, Louise ^{[1
]}

Drzewiecki, Jan ^{[1
]}

Fundo, Alexandra ^{[1
]}

Le Gall, Armelle ^{[1
]}

Gomez, Sylvie ^{[1
]}

Javaid, Hashim ^{[1
]}

Lence, Carlos Fenandez ^{[1
]}

Martin, Niall M. B. ^{[1
]}

Mydlowski, Chris ^{[1
]}

Smith, Graeme C. M. ^{[1
]}

机构：

[1] KuDos Pharmaceut Ltd, Cambridge CB4 0PE, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

poly(ADP-ribose) polymerase-1; PARP-1; PARP-2;

D O I：

10.1016/j.bmcl.2008.06.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.

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页码：3942 / 3945

页数：4

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