Abstract: The present invention relates to the design, synthesis, and biological study of multi-targeted Ubenimex pro-drug derivative. More particularly, provided in the present invention is a compound as shown by general structural formula (I) (wherein the definition of R is shown in the description). The derivative is a multi-targeted compound obtained by binding an aminopeptidase (APN/CD13) inhibitor, Ubenimex, with some anti-tumor drugs already on the market through an ester bond or amide bond, and is suitable for use as an anti-tumor drug for the treating various malignant tumors, and is especially suitable for treating various solid tumors.