C10‐Modified Artemisinin Derivatives: Efficient Heme‐Alkylating Agents

Discussion is reopened regarding C10-substituted derivatives of the peroxide-based antimalarial agent artemisinin (see picture); they are shown to react readily with iron(II)-heme to provide heme–drug adducts in high yields. Substitution or steric hindrance at C10 does not affect the reactivity of the peroxide bond and, thus, does not alter the ability of these powerful antimalarial drugs to alkylate heme.