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Issue 6, 2013
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Design and discovery of 4-anilinoquinazoline ureas as multikinase inhibitors targeting BRAF, VEGFR-2 and EGFR

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Abstract

4-Anilinoquinazoline ureas were envisaged according to the hybrid-design approach based upon two privileged pharmacophores in kinase drug discovery, i.e. 4-anilinoquinazoline and unsymmetrical diaryl urea. In our structure–activity relationships (SAR) campaign, title compounds were synthesized and profiled in biochemical assay for their kinase inhibitory activity. Title compounds 18–20 were found to be multikinase inhibitors with profound activity against BRAF, BRAF V600E, VEGFR-2 and EGFR. Molecular docking into DFG-out conformations of BRAF and VEGFR-2 suggested that they might be type II inhibitors.

Graphical abstract: Design and discovery of 4-anilinoquinazoline ureas as multikinase inhibitors targeting BRAF, VEGFR-2 and EGFR

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Article information


Submitted
28 Mar 2013
Accepted
26 Apr 2013
First published
01 May 2013

Med. Chem. Commun., 2013,4, 979-986
Article type
Concise Article

Design and discovery of 4-anilinoquinazoline ureas as multikinase inhibitors targeting BRAF, VEGFR-2 and EGFR

Q. Zhang, Y. Diao, F. Wang, Y. Fu, F. Tang, Q. You and H. Zhou, Med. Chem. Commun., 2013, 4, 979
DOI: 10.1039/C3MD00096F

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