Design, synthesis and biological evaluation of biphenylurea derivatives as VEGFR-2 kinase inhibitors (II)

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.

Graphical abstractIn an effort to discover potent VEGFR-2 inhibitors, a series of O-linked biphenylurea derivatives were designed and synthesized. The structural activity relationships led to identification of a potential VEGFR-2 inhibitor compound 39.Figure optionsDownload full-size imageDownload as PowerPoint slide