The invention provides diaryl urea compounds with anti-tumor activity as well as a preparation method and an application of the diaryl urea compounds. A structural formula of the compounds is shown in the specification, wherein R1 represents hydrogen or halogen groups, and R2 represents isobutyl or halogen groups. The compounds have good inhibition activity for VEGFR-2 (vascular endothelial growth factor-2) kinase and can block VEGFR-2 kinase induced signaling pathways and inhibit tumor cell proliferation and migration by inhibiting activity of VEGFR-2 kinase, so that the compounds can be applied to preparation of anti-tumor drugs. Besides, the preparation method of the compounds has the advantages that raw materials are easily available, reaction conditions are mild, a reaction process is simple to operate and used reagents are cheap.