Events 7th International Electronic Conference on Medicinal Chemistry

Event submissions

Published

10.3390/ECMC2021-11525

This submission belongs to the session S4. Fighting cancers of the event 7th International Electronic Conference on Medicinal Chemistry

Published date

03 Nov, 2021

Academic Editor

Jean Jacques Vanden Eynde

Citation

Elizaveta Dmitrievna Gladkova, Ivan Nechepurenko, Alexandra Zakharenko, Olga Luzina, Konstantin Volcho, Olga Lavrik, Nariman Salakhutdinov, Synthesis of berberine-based Tdp1 inhibitors, in Proceedings of 7th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2021, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2021-11525

Facebook

Twitter

Synthesis of berberine-based Tdp1 inhibitors

Elizaveta Dmitrievna Gladkova ^1,2

Ivan Nechepurenko ³

Alexandra Zakharenko ⁴

Olga Luzina ³

Konstantin Volcho ³

Olga Lavrik ^2,5

Nariman Salakhutdinov ⁶

1. N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, Russia

2. Novosibirsk State University

3. N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences

4. Novosibirsk Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences

5. Novosibirsk Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences

6. N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences

Abstract

An isoquinoline alkaloid berberine and its derivatives exhibit a wide range of biological activities including antibacterial, hypolipidemic, anticancer and other properties. We have shown for the first time that berberine derivatives are effective inhibitors of the human DNA repair enzyme tyrosyl-DNA phosphodiesterase (Tdp1), which opens the possibility to use them as an adjuvant component of chemotherapy.

We synthesised and analysed a few different types of berberine derivatives and studied their inhibitory activity. Berberine-based sulfonates and sultones have been shown to exhibit high inhibitory activity against Tdp1.

This work was supported by Russian Science Foundation (grant 19-13-00040)

Keywords

Berberine

berberubine

Tdp1

antitumor

alkaloid

DNA repair

Poster

Poster_Gladkova.pdf

Fluoroquinolone derivatives in the treatment of mycobacterium tuberculosis infection

Polyphenolic extracts from Viola x wittrockiana show antidiabetic properties and reduce fat storages of Caenorhabditis elegans