Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors

被引：47

作者：

Orvieto, Federica ^{[1
]}

Branca, Danila ^{[1
]}

Giomini, Claudia ^{[1
]}

Jones, Philip ^{[1
]}

Koch, Uwe ^{[1
]}

Ontoria, Jesus M. ^{[1
]}

Palumbi, Maria Cecilia ^{[1
]}

Rowley, Michael ^{[1
]}

Toniatti, Carlo ^{[1
]}

Muraglia, Ester ^{[1
]}

机构：

[1] IRBM, Merck Res Labs, I-00040 Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

PARP-1; inhibitor; Pyrazole; POLYMERASE PARP; CANCER; CELLS;

D O I：

10.1016/j.bmcl.2009.05.113

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1 inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.

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页码：4196 / 4200

页数：5

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