N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides:: Novel potent inhibitors of VEGF receptors I and II

被引：19
作者：
Kiselyov, AS
Piatnitski, E
Semenova, M
Semenov, VV
机构：
[1] Chem Divers Inc, Small Mol Drug Discovery, San Diego, CA 92121 USA
[2] ImClone Syst Inc, Dept Chem, New York, NY 10014 USA
[3] Russian Acad Sci, Inst Dev Biol, Moscow 119334, Russia
[4] Russian Acad Sci, ND Zelinskii Organ Chem Inst, Moscow 117913, Russia
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 03期
关键词：
vascular endothelial growth factor receptor 2; receptor tyrosine kinase; dual kinase inhibitor; angiogenesis; 4-(azolylethyl)thiazole-5-carboxamides;
D O I：
10.1016/j.bmcl.2005.10.058
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel potent derivatives of N-(aryl)-4-(azolylethyl)thiazole-5-carboxamides are described as inhibitors of vascular endothelial growth factor receptor 11 (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido pharmacophore, both dual and specific VEGFR-2 thiazoles were identified. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：602 / 606
页数：5
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