Issue 4, 2010
From the journal:

MedChemComm

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

Hiroyuki Nakamura,*a   Ryoji Horikoshi,a   Taikou Usuia  and  Hyun Seung Bana  

* Corresponding authors

a Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Toshima-ku, Tokyo 171-8588, Japan
E-mail: hiroyuyki.nakamura@gakushuin.ac.jp
Fax: +81 3 3986 0221
Tel: +81 3 5992 1029

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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Article information

DOI
https://doi.org/10.1039/C0MD00115E
Article type
Concise Article
Submitted
20 Jul 2010
Accepted
13 Aug 2010
First published
08 Sep 2010

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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