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Issue 44, 2013
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Design, synthesis, biological evaluation, and molecular modeling study of 4-alkoxyquinazoline derivatives as potential VEGFR2 kinase inhibitors

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Abstract

A series of novel 4-alkoxyquinazoline derivatives were prepared and synthesized and their biological activities were evaluated as potential inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2). Of these compounds, compound 3j demonstrated the most potent inhibitory activities against VEGFR2 tyrosine kinase and cell proliferation, the IC50 values of this compound reaching up to 2.72 nM and 0.35 μM, respectively, compared with Tivozanib (3.40 nM and 0.38 μM). The obtained results, along with a 3D-QSAR study and molecular docking that was used for investigating the probable binding mode, could provide an important basis for further optimization of compound 3j as a potential tyrosine kinase inhibitor.

Graphical abstract: Design, synthesis, biological evaluation, and molecular modeling study of 4-alkoxyquinazoline derivatives as potential VEGFR2 kinase inhibitors

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Publication details

The article was received on 31 May 2013, accepted on 08 Sep 2013 and first published on 10 Sep 2013


Article type: Paper
DOI: 10.1039/C3OB41136B
Org. Biomol. Chem., 2013,11, 7676-7686

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    Design, synthesis, biological evaluation, and molecular modeling study of 4-alkoxyquinazoline derivatives as potential VEGFR2 kinase inhibitors

    J. Sun, D. Li, J. Li, F. Fang, Q. Du, Y. Qian and H. Zhu, Org. Biomol. Chem., 2013, 11, 7676
    DOI: 10.1039/C3OB41136B

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