3,6-Bis(3-alkylguanidino)acridines as DNA-intercalating antitumor agents

► We have synthesized a new series of 3,6-bis(3-alkylguanidino)acridines 6a-e. ► These compounds showed strong DNA binding activity and they act as effective DNA-intercalating agents. ► The derivatives 6a and 6d showed mostly a transient cytostatic action. ► Derivative 6e proved to be both cytostatic and cytotoxic.