A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity:: Design, synthesis, and biological activity

被引：27

作者：

Hughes, Terry V. ^{[1
]}

Xu, Guozhang ^{[1
]}

Wetter, Steven K. ^{[1
]}

Connolly, Peter J. ^{[1
]}

Emanuel, Stuart L. ^{[1
]}

Karnachi, Prabha ^{[1
]}

Pollack, Scott R. ^{[1
]}

Pandey, Niranjan ^{[1
]}

Adams, Mary ^{[1
]}

Moreno-Mazza, Sandra ^{[1
]}

Middleton, Steven A. ^{[1
]}

Greenberger, Lee M. ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 17期

关键词：

EGFR; HER2; HER1; kinase; pyrimidine; quinazoline mimic; intramolecular hydrogen bond; restricted rotation; oxadiazole;

D O I：

10.1016/j.bmcl.2008.07.057

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2 kinase dependent cell lines will be discussed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4896 / 4899

页数：4

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