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Issue 4, 2010
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Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines

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Abstract

Boronic acid-containing 4-anilinoquinazolines were synthesized as selective inhibitors of EGFR and VEGFR2 tyrosine kinases. The substituted position of the boronic acid is essential for control of both kinase inhibitions, and the boronic acid substituted at the para position of the aniline moiety exhibited significant inhibition of VEGFR2 tyrosine kinase.

Graphical abstract: Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines

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The article was received on 20 Jul 2010, accepted on 13 Aug 2010 and first published on 08 Sep 2010


Article type: Concise Article
DOI: 10.1039/C0MD00115E
Citation: Med. Chem. Commun., 2010,1, 282-286
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    Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines

    H. Nakamura, R. Horikoshi, T. Usui and H. S. Ban, Med. Chem. Commun., 2010, 1, 282
    DOI: 10.1039/C0MD00115E

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