Recently, the anti-angiogenic therapy is a hot focus for antitumor research. The vascular endothelial growth factor (VEGF) is one of the most important angiogenesis stimulators. The vascular endothelial growth factor receptor (VEGFR) is high expressed in the new vessels of tumor tissues, so the antiangiogenic therapy aiming at VEGFR becomes an ideal treatment method. Besides the monoclonal antibody drug Avastin, the small-molecule inhibitors such as sunitinib and sorafenib are already widely used in the antitumor therapy aimed at VEGF and VEGFR. Moreover, it is also worth attention to some clinical drugs with potential market acceptance (vandetanib, cediranib, vatalanib, axtinib, et al). For the drugs on the market and VEGFR-targeted small-molecule inhibitors in clinical study, we roughly divided them into six kinds on structures including quinoline and quinazoline, pyridazine, indazole, imidazole, pyrrolo[2,3-d]pyrimidine, indole, and others. The recent studies of the biologyical function of VEGF and VEGFR and their representative small-molecule inhibitors are reviewed in this paper.