Ellipticines are potent antitumor agents whose mechanism of action is considered to be based mainly on DNA intercalation and/or inhibition of topoisomerase II. Targeting of the ellipticine drugs specifically on tumor cells has been the goal of many studies. A survey of such targeting of ellipticines on tumor cells and definition of the structural requirements for receptor-targeted drugs are given in the present article. Targeted cytotoxic drugs consisting of heptagastrin, modified enkephalin, estradiol, saccharides, lipoproteins and human serum albumin linked to ellipticines, designed and prepared by many authors are shown and their efficiencies in tumors are discussed.