The invention discloses a scutellarein derivative shown in a formula I, a preparation method of the scutellarein derivative, and application of the scutellarein derivative in preparing anti-tumor drugs. The preparation method comprises the following steps of using scutellarein as an initiating raw material, and synthesizing a series of scutellarein derivatives with an A ring benzodioxane structure, a B ring 4apostrophe-position connected lipid-soluble group and a water-soluble group. The preparation method has the advantages that the synthesizing method is simple, and the operability and reaction yield rate are better. The scutellarein derivative has the advantages that the activity for inhibiting proliferation of multiple tumor cells is realized, and the activity of the scutellarein derivative is better than or equivalent to the activity of scutellarein; the scutellarein derivative is expected to develop into the anti-tumor drugs. (The formula I is shown in the description).