Structure-driven HtL: Design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity

被引：45

作者：

Stocks, MJ

Barber, S

Ford, R

Leroux, F

St-Gallay, S

Teague, S

Xue, YF

机构：

[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Dept Phys & Metab Sci, Loughborough LE11 5RH, Leics, England

[3] AstraZeneca R&D, Struct Chem Lab, S-43183 Molndal, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 14期

关键词：

aminoindazole; C-jun N-terminal kinase; inhibitors; bioavailable;

D O I：

10.1016/j.bmcl.2005.05.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and synthesis of a new series of c-Jun N-terminal kinase inhibitors are reported. The novel series of substituted amino indazoles were designed based on a combination of hits from high-throughput screening and X-ray crystal structure information of the compounds crystallised into the JNK-1 ATP binding site. C 2005 Elsevier Ltd. All rights reserved.

引用

页码：3459 / 3462

页数：4

共 27 条

[1] The c-Jun amino-terminal kinase pathway is preferentially activated by interleukin-1 and controls apoptosis in differentiating pancreatic β-cells [J].