Synthesis and antitumor activity of daunorubicin conjugates with of 3,4-methylendioxybenzaldehyde

Bioorg Med Chem Lett. 2019 Oct 1;29(19):126617. doi: 10.1016/j.bmcl.2019.08.021.

Aleksandra A Moiseeva ¹, Oleg I Artyushin ¹, Lada V Anikina ², Valery K Brel ³

Affiliations

1 A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, Moscow 119991, Russia.
2 Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severny pr., Chernogolovka 142432, Russia.
3 A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, Moscow 119991, Russia. Electronic address: v_brel@mail.ru.

PMID: 31431363 DOI: 10.1016/j.bmcl.2019.08.021

Abstract

The design of hybrid (chimeric) molecules containing two different pharmacophores connected via a spacer (linker) is a promising approach to the functionalization of natural compounds and potentially of drug molecules. These are important examples for the use of this approach with anthracycline Antibiotics. The use of this methodology may help to eliminate some of the drawbacks of anthracycline drugs, e.g., high cardiotoxicity and MDR development.

Keywords

Anthracycline antibiotics; Anticancer activity; Antitumor conjugates; Daunorubicin.

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