Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable

被引：7

作者：

Buttar, David ^{[1
]}

Edge, Mike ^{[1
]}

Emery, Steve C. ^{[1
]}

Fitzek, Martina ^{[1
]}

Forder, Cheryl ^{[1
]}

Griffen, Alison ^{[1
]}

Hayter, Barry ^{[1
]}

Hayward, Chris F. ^{[1
]}

Hopcroft, Philip J. ^{[1
]}

Luke, Richard W. A. ^{[1
]}

Page, Ken ^{[1
]}

Stawpert, John ^{[1
]}

Wright, Andy ^{[1
]}

机构：

[1] AstraZeneca, Canc & Infect Res Area, Mereside, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 16期

关键词：

angiogenesis; kinase; Tie-2; inhibitor; pyrimidine; imidazole; alkene;

D O I：

10.1016/j.bmcl.2008.06.106

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tie-2 is a receptor tyrosine kinase which is involved in angiogenesis and thereby growth of human tumours. The discovery and SAR of a novel class of imidazole-vinyl-pyrimidine kinase inhibitors, which inhibit Tie-2 in vitro is reported. Their synthesis was carried out by condensation of imidazole aldehydes with methyl pyrimidines. These compounds are lead-like, with low molecular weight, good physical properties and oral bioavailability. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4723 / 4726

页数：4

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