Design of anthracyclines with extremely high cytotoxic properties

Abstract

Chemotherapy with anthracycline antibiotics is a common treatment of tumours of various etiologies. Creation of highly effective cytostatics based on daunorubicin is possible by applying the method of reductive amination using polyalkoxybenzaldehydes. The obtained derivatives of anthracycline structure are up to 500 times more potent compared with daunorubicin due to the increased affinity to DNA, which is confirmed by the data of extensive biological assays and the results of molecular modeling.