The present invention relates to a benzoindazole derivative, a preparation method and applications thereof, wherein the structural general formula of the benzoIndazole derivative is defined in the specification, R1 is selected from hydrogen, alkoxy, halogen, nitro, amino, and an oxygen substituent, R2 is selected from hydrogen and alkoxy, and R3 is selected from hydrogen, straight chain alkyl, substituted alkyl, aryl, carboxylic acid, and carboxylic acid ester. According to the present invention, the benzoindazole derivative can inhibit tubulin polymerization, has antitumor activity in leukemia, non-small cell lung cancers, colon cancers, central nervous system neoplasms, melanoma, ovarian cancers, kidney cancers, prostate cancers, breast cancers and the like, and has low cytotoxicity.