Design,synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors(Ⅰ)

Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer.In this study,we describe the design,synthesis,and biological evaluation of a series of O-linked indoles as potent inhibitors of VEGFR-2.Among these compounds,18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays,with IC_(50) value of3.8 nmol/L Kinase selectivity profiling revealed that 18 was a multitargeted inhibitor,and it also exhibited good potency against VEGFR-1,PDCFR-α and β.