Design of anthracyclines with extremely high cytotoxic properties

Author:

Moiseeva Aleksandra A.1,Artyushin Oleg I.1,Anikina Lada V.2,Globa Anastasiya A.2,Klemenkova Zinaida S.1,Andreev Maxim V.1,Radchenko Eugene V.3,Palyulin Vladimir A.3,Brel Valery K.1

Affiliation:

1. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilova St. 28, bld. 1, Moscow, 119991, Russia

2. Institute of Physiologically Active Compounds of the FSBIS of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the RAS

3. Lomonosov Moscow State University

Abstract

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.

Publisher

Research Square Platform LLC

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