Journal Article

Design of New Daunorubicin Derivatives with High Cytotoxic Potential

Andreev, Maxim V., Globa, Anastasiya A., Aleksandrova, Yulia R., Artyushin, Oleg I., Chubarev, Vladimir N., Syzdykbayev, Marat I., Brel, Valery K., Radchenko, Eugene V., Appazov, Nurbol O., Klemenkova, Zinaida S., Palyulin, Vladimir A., Kalashnikova, Aleksandra A., Toibazarova, Altynkul B., Anikina, Lada V., Neganova, Margarita E.

2025

Overview

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.

• Publisher: MDPI AG,MDPI
• Subject: Aldehydes / Antibiotics / Antibiotics, Antineoplastic - chemical synthesis / Antibiotics, Antineoplastic - chemistry / Antibiotics, Antineoplastic - pharmacology / Antimitotic agents / Antineoplastic agents / Antineoplastic Agents - chemistry / Antineoplastic Agents - pharmacology / Cancer / Carbohydrates / Cell cycle / Cell Cycle - drug effects / Cell Line, Tumor / Cell Proliferation - drug effects / Cell Survival - drug effects / Chemotherapy / Cytotoxicity / Daunorubicin / Daunorubicin - analogs & derivatives / Daunorubicin - chemical synthesis / Daunorubicin - chemistry / Daunorubicin - pharmacology / Drug Design / Drugs / Enzymes / Glycolysis - drug effects / Humans / Mutation / Toxicity