Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors

被引：25

作者：

Liu, M ^{[1
]}

Xin, ZL ^{[1
]}

Clampit, JE ^{[1
]}

Wang, SY ^{[1
]}

Gum, RJ ^{[1
]}

Haasch, DL ^{[1
]}

Trevillyan, JM ^{[1
]}

Abad-Zapatero, C ^{[1
]}

Fry, EH ^{[1
]}

Sham, HL ^{[1
]}

Liu, G ^{[1
]}

机构：

[1] Abbott Labs, Metab Dis Res, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

JNK; diabetes; obesity; pyrazoloquinolinones;

D O I：

10.1016/j.bmcl.2006.02.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure-activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2590 / 2594

页数：5

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