Synthesis of berberine-based Tdp1 inhibitors

Elizaveta Gladkova; Ivan Nechepurenko; Alexandra Zakharenko; Olga Luzina; Konstantin Volcho; Olga Lavrik; Nariman Salakhutdinov

doi:10.3390/ECMC2021-11525

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Synthesis of berberine-based Tdp1 inhibitors

Elizaveta Dmitrievna Gladkova

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Nariman Salakhutdinov

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

Academic Editor: Jean Jacques Vanden Eynde

Published: 03 November 2021 by MDPI in 7th International Electronic Conference on Medicinal Chemistry session Fighting cancers

https://doi.org/10.3390/ECMC2021-11525

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

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