Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors

被引：37

作者：

Cao, Jingrong ^{[1
]}

Gao, Huai ^{[1
]}

Bemis, Guy ^{[1
]}

Salituro, Francesco ^{[1
]}

Ledeboer, Mark ^{[1
]}

Harrington, Edmund ^{[1
]}

Wilke, Susanne ^{[1
]}

Taslimi, Paul ^{[1
]}

Pazhanisamy, S. ^{[1
]}

Xie, Xiaoling ^{[1
]}

Jacobs, Marc ^{[1
]}

Green, Jeremy ^{[1
]}

机构：

[1] Vertex Pharmaceut Inc, Cambridge, MA 02139 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期

关键词：

JNK3; inhibitors; MAP kinase; Isatin; SELECTIVE INHIBITORS; JUN; POTENT; DISCOVERY;

D O I：

10.1016/j.bmcl.2009.03.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-benzylated isatin oximes were developed as inhibitors of the mitogen-activated kinase, JNK3. X-ray crystallographic structures aided in the design and synthesis of novel, selective compounds, that inhibit JNK3, but not p38 MAP kinase and provided key insights into understanding the behavior of gatekeeper residue methionine-146 in determining target selectivity for this series. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2891 / 2895

页数：5

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