Journal
BIOORGANIC CHEMISTRY
Volume 56, Issue -, Pages 16-26Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2014.05.010
Keywords
VEGFR-2; Kinase; Type-II; Quinoxaline; Docking study
Funding
- Science and Technology Development Fund (STDF) at the Faculty of Pharmacy Ain Shams University [5251]
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In an effort to develop ATP-competitive VEGFR-2 selective inhibitors, a series of new quinoxaline-based derivatives was designed and synthesized. The target compounds were biologically evaluated for their inhibitory activity against VEGFR-2. The design of the target compounds was accomplished after a profound study of the structure activity relationship (SAR) of type-II VEGFR-2 inhibitors. Among the synthesized compounds, 1-(2-((4-methoxyphenyl)amino)-3-oxo-3,4 dihydroquinoxalin-6-yl)-3-phenylurea (VIIa) displayed the highest inhibitory activity against VEGFR-2. Molecular modeling study involving molecular docking and field alignment was implemented to interpret the variable inhibitory activity of the newly synthesized compounds. (C) 2014 Elsevier Inc. All rights reserved.
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