To improve water solubility of 1,4-dihydroxy-9,10-anthraquinone moiety, 23 of 2-(1-aminoacetylalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives, which contain nitrogen atom, were synthesized. Of the synthesized compounds, 18 compounds were more cytotoxic on L1210 cells than 2-(1-acetyloxyalkyl)-1,4-dihydroxy-9,10-anthraquinone as comparative structure. This result might be due to the increased hydrophilicity of the compounds.