The effect of the replacement of amino groups, attached to the anthraquinone ring in [(aminoalkyl)amino]-anthraquinones, by an amido function on DNA binding, cytotoxicity, and antileukemic activity has been studied. The corresponding 1,4-bis(aminoalkanamido)-9,10-anthracenediones have been synthesized and examined. It has been concluded that such modification does not exclude the DNA binding and cytotoxicity of mentioned compounds but decreases or abolishes the in vivo antileukemic activity.