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

Authors
Journal
Tetrahedron Letters
0040-4039
Publisher
Elsevier
Publication Date
Volume
47
Issue
17
Identifiers
DOI: 10.1016/j.tetlet.2006.02.119
Keywords
  • Biotin-Tagged Photoaffinity Probe
  • Vascular Endothelial Growth Factor Receptors
  • Ligand–Receptor Interactions
  • Inhibitor
  • Trifunctional Probe

Abstract

Abstract 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 IC 50 values of 29.7, 33.3, and 37.7 μM, respectively. Moreover, we identified the interaction of 3b with VEGFR-2 in photoaffinity labeling experiment using HUVE cells.

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