Isoxazole-linked 7-hydroxycoumarin--2,6-dimethylheptane conjugates as inhibitors of TDP1 enzyme
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 IC<sub>50</sub> values in the low micromolar or submicromolar concentration range.
Authors
- Olga I. Lavrik (ORCID: https://orcid.org/0000-0001-5980-8889)
- Dmitry O. Tsypyshev (ORCID: https://orcid.org/0000-0003-4551-0226)
- Evgeniy V. Kondrashov (ORCID: https://orcid.org/0000-0002-0599-1128)
- Т. М. Хоменко (ORCID: https://orcid.org/0009-0007-5702-3595)
- Константин П. Волчо (ORCID: https://orcid.org/0000-0002-4083-9324)
- Нариман Ф. Салахутдинов (ORCID: https://orcid.org/0000-0001-8512-4309)
- Alexandra L. Zakharenko
- Maria V. Podurina
Institutions
- Novosibirsk State University (RU)
- Institute of Chemical Biology and Fundamental Medicine (RU)
- Novosibirsk Institute of Organic Chemistry (RU)
- A.E. Favorsky Irkutsk Institute of Chemistry (RU)
- Siberian Branch of the Russian Academy of Sciences (RU)
Publication Details
- Journal
- Mendeleev Communications
- Published
- 2025-01-01
- DOI
- https://doi.org/10.71267/mencom.7704
- Primary Topic
- Carbohydrate Chemistry and Synthesis
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Ministry of Education and Science of the Russian Federation
- Russian Science Foundation