2-((1H-azol-1-yl)methyl)-N-arylbenzamides:: Novel dual inhibitors of VEGFR-1/2 kinases

被引：17
|
作者：
Kiselyov, AS
Semenova, M
Semenov, VV
Piatnitski, E
机构：
[1] Chem Divers Inc, Small Mol Drug Discovery, San Diego, CA 92121 USA
[2] Russian Acad Sci, Inst Dev Biol, Moscow 119334, Russia
[3] Russian Acad Sci, ND Zelinskii Organ Chem Inst, Moscow 117913, Russia
[4] ImClone Syst, Small Mol Drug Discovery, New York, NY 10014 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期
关键词：
vascular endothelial growth factor receptor 2; receptor tyrosine kinase; dual kinase inhibitor; angiogenesis; 2-((1H-azol-1-yl)methyl)-N-arylbenzyl amides;
D O I：
10.1016/j.bmcl.2005.11.105
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel potent derivatives of (azol-1-yl)methyl-N-arylbenzamides with improved solubility (>3 mM) are described as ATP-competitive inhibitors of vascular endothelial growth factor receptor 2 (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in the enzymatic assay. The compounds also inhibit the related tyrosine kinase, VEGFR-1, with similar potencies. Several compounds containing bulky lipophilic substituents at the benzamide pharmacophore yielded 10- to 17-fold selectivity for the VEGFR-2 versus VEGFR-1 kinase. (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1726 / 1730
页数：5
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