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In an effort to discover potent VEGFR-2 inhibitors, a series of 2,4 or 4,6-disubstituted <b>O</b>-linked indoles derivatives were designed and synthesized. The structural activity relationships led to identification of a potential VEGFR-2 inhibitor compound <b>18</b>.<br>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 <b>O</b>-linked indoles as potent inhibitors of VEGFR-2. Among these compounds, <b>18</b> showed significant anti-angiogenesis activities <b>via</b> VEGFR-2 in enzymatic proliferation assays, with IC50 value of 3.8 nmol/L. Kinase selectivity profiling revealed that <b>18</b> was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-<b>α</b> and <b>β</b>.