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

A series of 4-aminoquinazoline derivatives based inhibitors of VEGFR-2 tyrosine kinases were synthesized and identified. Some of them exhibited significant VEGFR-2 inhibitory activity. Of all the studied compounds, compounds 1h, 1n, 1o exhibited the most potent inhibitory activity. The lead compound 1h also showed in vivo activity against HepG2 human tumor xenograft model in BALB/c-nu mice.