摘要
Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.
Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.
基金
the National Natural Science Foundation of China (Nos. 81273365, 81173080, 81321092)
National Science & Technology Major Project ‘‘Key New Drug Creation and Manufacturing Program’’ (Nos. 2012ZX09103101-024, 2014ZX09304002-008-001)
Chinese National Programs for High Technology Research and Development (No. 2012AA020302)
the Shanghai Science and Technology Commission (No. 12DZ1930802) for their financial support
