Design and synthesis of novel photoaffinity reagents for labeling VEGF receptor tyrosine kinases

被引：12
|
作者：
Han, SY [1 ]
Choi, SH [1 ]
Kim, MH [1 ]
Lee, WG [1 ]
Kim, SH [1 ]
Min, YK [1 ]
Kim, BT [1 ]
机构：
[1] Korea Res Inst Chem Technol, Bioorgan Sci Div, Taejon 305606, South Korea
来源：
TETRAHEDRON LETTERS | 2006年 / 47卷 / 17期
关键词：
biotin-tagged photoaffinity probe; vascular endothelial; growth factor receptors; ligand-receptor interactions; inhibitor; trifunctional probe;
D O I：
10.1016/j.tetlet.2006.02.119
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Novel biotin-tagged photoaffinity probes based on a trifunctional tertiary amine scaffold were synthesized and evaluated as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Probes 3a-c inhibit VEGF induced proliferation in HUVE cells, with IC50 values of 29.7, 33.3, and 37.7 mu M, respectively. Moreover, we identified the interaction of 3b with VEGFR-2 in photoaffinity labeling experiment using HUVE cells. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2915 / 2919
页数：5
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