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Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme

Dmitry Olegovich Tsypyshev 1
Dmitry Olegovich Tsypyshev
, 
Alexandra Leonidovna Zakharenko 2
Alexandra Leonidovna Zakharenko
, 
Maria V. Podurina 2, 3
Maria V. Podurina
, 
Tatiana Mikhailovna Khomenko 1
Tatiana Mikhailovna Khomenko
, 
Evgenii Vladimirovich Kondrashov 4
Evgenii Vladimirovich Kondrashov
, 
Olga Ivanovna Lavrik 2, 3
Olga Ivanovna Lavrik
, 
Konstantin Petrovich Volcho 1
Konstantin Petrovich Volcho
, 
Nariman Faridovich Salakhutdinov 1
Nariman Faridovich Salakhutdinov
2 Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russian Federation
4 A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russian Federation
10.71267/mencom.7704
Published 2025-05-21
Communication , Volume 35, Issue 4, 444-446
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Tsypyshev D. O. et al. Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme // Mendeleev Communications. 2025. Vol. 35. No. 4. pp. 444-446.
GOST all authors (up to 50) Copy
Tsypyshev D. O., Zakharenko A. L., Podurina M. V., Khomenko T. M., Kondrashov E. V., Lavrik O. I., Volcho K. P., Salakhutdinov N. F. Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme // Mendeleev Communications. 2025. Vol. 35. No. 4. pp. 444-446.
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TY - JOUR
DO - 10.71267/mencom.7704
UR - https://mendcomm.colab.ws/publications/10.71267/mencom.7704
TI - Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme
T2 - Mendeleev Communications
AU - Tsypyshev, Dmitry Olegovich
AU - Zakharenko, Alexandra Leonidovna
AU - Podurina, Maria V.
AU - Khomenko, Tatiana Mikhailovna
AU - Kondrashov, Evgenii Vladimirovich
AU - Lavrik, Olga Ivanovna
AU - Volcho, Konstantin Petrovich
AU - Salakhutdinov, Nariman Faridovich
PY - 2025
DA - 2025/05/21
PB - Mendeleev Communications
SP - 444-446
IS - 4
VL - 35
ER -
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@article{2025_Tsypyshev,
author = {Dmitry Olegovich Tsypyshev and Alexandra Leonidovna Zakharenko and Maria V. Podurina and Tatiana Mikhailovna Khomenko and Evgenii Vladimirovich Kondrashov and Olga Ivanovna Lavrik and Konstantin Petrovich Volcho and Nariman Faridovich Salakhutdinov},
title = {Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme},
journal = {Mendeleev Communications},
year = {2025},
volume = {35},
publisher = {Mendeleev Communications},
month = {May},
url = {https://mendcomm.colab.ws/publications/10.71267/mencom.7704},
number = {4},
pages = {444--446},
doi = {10.71267/mencom.7704}
}
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Tsypyshev, Dmitry Olegovich, et al. “Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme.” Mendeleev Communications, vol. 35, no. 4, May. 2025, pp. 444-446. https://mendcomm.colab.ws/publications/10.71267/mencom.7704.

Keywords

antitumor
biological activity.
coumarin
isoxazole
saturated terpenoids
synthesis
TDP1

Abstract

Novel monoterpenoid derivatives of 7-hydroxycoumarine containing an isoxazole linker were synthesized, 2,3-dichloropropene having been the synthetic equivalent of propargyl chloride at the step of isoxazole moiety construction. The conjugates demonstrated promising inhibitory activity against TDP1, an important target for complex anticancer therapy, with IC50 values in the low micromolar or submicromolar concentration range.

Funders

Russian Science Foundation
24-13-00134