The invention provides a preparation method of compounds with the structure represented by general formula 1, and an application of the compounds in the preparation of antitumor drugs. The compounds are prepared through ester bond condensation of a 3th hydroxyl group of an anticancer lead compound TOA (patent 201110055102.X) and a carboxyl group of amino acids; and the compounds have a more substantial inhibition effect on liver cancer, colorectal carcinoma, cervical carcinoma and stomach cancer cell lines than the TOA, have smaller toxicity to normal cells than cis-platinum, have obviously better water solubility than the TOA, and are especially suitable for preparing antitumor treatment drugs.