STUDY OF THE ABILITY OF A NEW USNIC ACID DERIVATIVE TO INHIBIT TDP1 AND TDP2, AND SENSITISE THE EFFECT OF ANTITUMOUR DRUGS

STUDY OF THE ABILITY OF A NEW USNIC ACID DERIVATIVE TO INHIBIT TDP1 AND TDP2, AND SENSITISE THE EFFECT OF ANTITUMOUR DRUGS Full article

Journal

ХИМИЯ В ИНТЕРЕСАХ УСТОЙЧИВОГО РАЗВИТИЯ
ISSN: 0869-8538 , E-ISSN: 1817-1818

Output data

Year: 2023, Volume: 31, Number: 6, Pages: 707-714 Pages count : 8 DOI: 10.15372/CSD2023520

Tags

USNIC ACID, USNIC ACID DERIVATIVES, TDP1 INHIBITOR, ANTI-TUMOR THERAPY, SENSIBILISATION, TEMOZOLOMIDE, OLAPARIB

Authors

FILIMONOV A.S. ¹ , ZAKHARENKO A.L. ² , CHEPANOVA A.A. ² , LUZINA O.A. ¹ , DYRKHEEVA N.S. ² , SALAKHUTDINOV N.F. ¹ , LAVRIK O.I. ²

Affiliations

1	Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences
2	Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences

A new usnic acid derivative containing cyanoethyl and isoniazid fragments is synthesised. The compound inhibits the activity of DNA repair enzyme Tdp1 with IC50 = 1.2 μM, is inactive against Tdp2 and does not affect cell survival for a panel of passaged cell lines in the concentration range up to 20 μM. It is shown that the compound in combinations with the certain concentrations of antitumour drugs can sensitise the effect of antitumour drugs olaparib and temozolomide on some cell lines.

FILIMONOV A.S. , ZAKHARENKO A.L. , CHEPANOVA A.A. , LUZINA O.A. , DYRKHEEVA N.S. , SALAKHUTDINOV N.F. , LAVRIK O.I.
STUDY OF THE ABILITY OF A NEW USNIC ACID DERIVATIVE TO INHIBIT TDP1 AND TDP2, AND SENSITISE THE EFFECT OF ANTITUMOUR DRUGS
ХИМИЯ В ИНТЕРЕСАХ УСТОЙЧИВОГО РАЗВИТИЯ. 2023. V.31. N6. P.707-714. DOI: 10.15372/CSD2023520 WOS РИНЦ

Филимонов А.С. , Захаренко А.Л. , Чепанова А.А. , Лузина О.А. , Дырхеева Н.С. , Салахутдинов Н.Ф. , Лаврик О.И.
Изучение ингибирующей Tdp1 и Tdp2 способности и сенсибилизирующих действие противоопухолевых препаратов свойств нового производного усниновой кислоты
ХИМИЯ В ИНТЕРЕСАХ УСТОЙЧИВОГО РАЗВИТИЯ. 2023. Т.31. С.728-736. DOI: 10.15372/KhUR2023520 РИНЦ

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