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

页码：2915 / 2919

页数：5

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