The invention relates to the technical field of medicine, and relates to a type of compounds with antitumor activities, and a preparation method and an application thereof. The compounds have a structural general formula represented below. R1 is alkyl group, heterocyclic group, substituted phenyl group, substituted alicyclic group, or aliphatic heterocyclic group, wherein the substituent is 2,3-ethylenedioxy, 3,4-ethylenedioxy, 2,3-methylenedioxy, or 3,4-methylenedioxy; or all-site-substituted hydrogen, alkyl, alkoxy, halogen, amino, hydroxyl, trifluoromethyl, formate, and the like. R2 is heterocyclic group or substituted phenyl group, wherein the phenyl substituent is 2,3-ethylenedioxy, 3,4-ethylenedioxy, 2,3-methylenedioxy, or 3,4-methylenedioxy; or all-site-substituted hydrogen, alkyl, alkoxy, halogen, amino, hydroxyl, trifluoromethyl, formate, and the like. The compounds provided by the invention have substantial tumor cytotoxic effect and broad-spectrum kinase inhibitory activity, and can be used in preparing antitumor medicines.