Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups

被引：21
|
作者：
Gaudette, Frederic [1 ]
Raeppel, Stephane [1 ]
Nguyen, Hannah [2 ]
Beaulieu, Normand [2 ]
Beaulieu, Carole [2 ]
Dupont, Isabelle [2 ]
Macleod, A. Robert [2 ]
Besterman, Jeffrey M. [2 ]
Vaisburg, Arkadii [1 ]
机构：
[1] MethylGene Inc, Dept Med Chem, Montreal, PQ H4S 2A1, Canada
[2] MethylGene Inc, Dept Cell Biol & Pharmacol, Montreal, PQ H4S 2A1, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期
关键词：
VEGFR2/KDR; c-Met; RTK inhibitors; Amide isostere; Angiogenesis; PARTIALLY MODIFIED RETRO; C-MET; CATHEPSIN-K; CANCER; GROWTH; TARGET; ANGIOGENESIS;
D O I：
10.1016/j.bmcl.2009.12.099
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：848 / 852
页数：5
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