Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase.

Bing Yu, Li-da Tang, Yi-Liang Li, Shu-Hui Song, Xiao-Liang Ji, Mu-Sen Lin, Chun-Fu Wu

Index: Bioorg. Med. Chem. Lett. 22 , 110-4, (2012)

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Abstract

We report herein the design and synthesis of novel 4-aminoquinazoline derivatives based on the inhibitors of VEGFR-2 tyrosine kinases. The VEGFR-2 inhibitory activities of these newly synthesized compounds were also evaluated and compared with that of ZD6474. We found that most of target compounds had good inhibitory potency. In particular, compounds 1h, 1n and 1o were found to be 6, 2 and 2-fold more potent than the positive control ZD6474. The leading compound 1h also showed an in vivo activity against HepG2 human tumor xenograft model in BALB/c-nu mice.Copyright © 2011 Elsevier Ltd. All rights reserved.