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Heme, resulting from hemoglobin digestion by the malaria parasite is one of the main target of antimalarial drugs like chloroquine and artemisinin. This later molecule contains a trioxane which is activated by the reduced form of heme to generate a strong alkylating agent able to react with heme itself. Taking advantage of these studies, we prepared new antimalarial drugs, trioxaquines, containing a trioxane motif covalently linked to an aminoquinoline.