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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.
Inhibition of VEGFR-2 signaling pathway has 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. Amm these compounds, 18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays, with IC 50 (50) value of 3.8 nmol / L Kinase selectivity profiling revealed 18 that a multitargeted inhibitor, and it also exhibiting good potency against VEGFR-1, PDCFR-α and β.