Alkylation of heme by the antimalarial drug artemisinin

Abstract
The peroxide function of artemisinin has been activated by iron(II)-heme generated in situ from iron(III)-protoporphyrin-IX and glutathione, a biologically relevant reductant. In mild conditions, this reaction produced a high yield (85%) of heme derivatives alkylated at α-, β-, and δ-meso positions by a C4-centered radical derived from artemisinin.

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