RUS  ENG
Full version
JOURNALS // Mendeleev Communications // Archive

Mendeleev Commun., 2025 Volume 35, Issue 4, Pages 444–446 (Mi mendc7260)

Communications

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

D. O. Tsypysheva, A. L. Zakharenkob, M. V. Podurinabc, T. M. Khomenkoa, E. V. Kondrashovd, O. I. Lavrikbc, K. P. Volchoa, N. F. Salakhutdinova

a N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russian Federation
b Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russian Federation
c Department of Natural Sciences, Novosibirsk State University, 630090 Novosibirsk, Russian Federation
d A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russian Federation

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.

Keywords: coumarin, isoxazole, saturated terpenoids, TDP1, antitumor, synthesis, biological activity.

Received: 09.12.2024
Accepted: 07.02.2025

Language: English

DOI: 10.71267/mencom.7704



Bibliographic databases:


© Steklov Math. Inst. of RAS, 2025