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 IC₅₀ values in the low micromolar or submicromolar concentration range.