Anthracycline antibiotics are among the most effective chemotherapy agents currently in use for cancer treatment; however irreversible cardiac damage is a major dose-limiting toxicity, restricting life-time cumulative dose. Besides, the therapeutic activity of many drugs of this class is low if tumor cells express multidrug resistance mediated by a decreased drug accumulation. With the aim of decreasing toxic side effects and also of finding drugs effective in treatment tumors resistant to existing antitumor drugs, investigations are being carried out widely on the synthesis of different analogues of anthracycline antibiotics and the methods of tumor targeted delivery. The design of new generation potential anticancer agents based on known structural principles was found to produce compounds with significantly increased chemotherapeutical indexes.