Abstract：Tumorangiogenesis is an important process of tumor growth and metastasis. Vascular endothelial growth factor (VEGF) and their receptors (VEGFR1, 2, 3) regulate the proliferation and migration of endothelial cells and are highly expressed in many tumors. The inhibition of VEGFR has become an effective therapy for many cancers. VEGFR2 plays an important role in tumor angiogenesis. VEGFR2 phosphorylation is a key factor in the mechanism of VEGF signaling pathway and cancer angiogenic process. VEGF signaling pathways can be blocked by antibodies and small molecules binding to VEGF and interfering with different VEGFR domains. Many small molecule VEGFR2 inhibitors, most of which are multi-target inhibitors, have been developed by researchers and approved by FDA. This review reports small molecule VEGFR2 inhibitors launched and in late-phase clinical study, their activities, recent clinical trials and makes a brief analysis of their structure-activity relationship (SAR). Future research may take advantage of multi-target inhibitors while avoiding their side effects.
