In order to obtain novel lead compounds with high efficacy, low toxicity and minimum of side effects, using chrysin(5, 7-dihydroxyflavone) with very broad biological activities as a starting material, four intermediates 7-O-carboxyalkylation chrysin derivatives(6-9) were synthesized by halogenation and hydrolysis. Four glycine methyl ester derivatives containing chrysin(12-15) were synthesized when the four intermediates above condensated with glycine methyl ester hydrochloride using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDCI), N-hydroxybenzotriazole(HOBt) and 4-dimethylamiopryidine(DMAP) as a coupling reagent. And then the corresponding glycine derivatives of chrysin(16-19) were obtained by hydrolysis under conditions of room temperature and pH 10-11. The structures of the target compounds were assigned by <sup>1</sup>H NMR, <sup>13</sup>C NMR, IR and MS. Taking cisplatin as a reference substance, the in vitro antitumor activity tests for target compounds against human hepatocellular carcinoma HepG2 cells and gastric carcinoma MGC-803 cells were carried out by MTT method. The results of primary pharmacological tests indicated that five compounds(14-16, 18, 19) possessed the more potent antitumor activity than chrysin in vitro. What's more, the antitumor activity of compound 18(IC<inf>50</inf>=4.36 μmol/L) against MGC-803 cells was better than the positive reference compound cisplatin(IC<inf>50</inf>=4.40 μmol/L).