A convenient approach to modify bioactive substrates such as daunorubicin, cytisine, and camphecene with a pentafluorosulfanylvinyl moiety have been suggested. F₅S-CH = CH derivatives of daunorubicin were obtained by acylation with reactive 4-nitrophenyl-4-(pentafluoro-λ⁶-sulfanyl)alkenyl carbonates, while the corresponding conjugates of anthracycline antibiotic daunorubicin, alkaloid cytisine and camphecene were synthesized using a click chemistry procedure.

Chemotherapy with anthracycline antibiotics is a common method of treating tumors of various etiologies. To create more highly effective cytostatics based on daunorubicin, we used the method of reductive amination using polyalkoxybenzaldehydes. The obtained derivatives of the anthracycline structure have much greater cytotoxicity compared to daunorubicin due to increased affinity for DNA, the ability to disrupt the cell cycle, and their inhibition of the glycolysis process, which is confirmed by data from extensive biological studies and the results of molecular modeling.

One-step reductive amination of aromatic aldehydes using an anthracycline antibiotic daunorubicin resulted in the preparation of its new N-derivatives, which are of interest as potential antitumor drugs.