ObjectiveSynthesis and anti-tumor activity of 6-chloro/methyl-2/3-arylquinoxaline derivatives on SGC-7901 and HepG2 cells have been studied.MethodsTarget compounds(3c-1~7m-1) were synthesized by cyclization,chlorination, and nucleophilic substitution reactionwith 4-chloro/methylbenzene-1,2-diamine and 1,2-dione compounds(diethyl oxalate) as the starting materials.The antitumor activity of 15 new compounds was evaluated by MTT assay.ResultsTarget compounds can be synthesized and all of them were further characterized by IR and 1H NMR.The results showed that the inhibiting rate of target compounds on SGC-7901 was greater than that of them on HepG2 cells, and inhibition effect of 6-chloro-2/3-arylquinoxaline derivatives to SGC-7901 cells was better than that of 6-methyl-2/3-arylquinoxaline derivatives.The inhibiting rate of 6-chloro-2/3-arylquinoxaline derivatives (5c-1) and 6-methyl-2/3-arylquinoxaline derivatives (7m-1) was 2.02 and 0.001 6 μg/mL, respectively.ConclusionAnti-tumor activity of target compounds(5c-1, 7m-1) on SGC-7901 was good.Therefore, the structure of 6-chloro/methyl-2/3-arylquinoxaline derivatives can be optimized to promote the anticancer activity of quinoxaline derivatives.