Alkylation of heme by the antimalarial drug artemisinin
Anne Robert1, Yannick Coppel, Bernard Meunier
1Laboratoire de Chimie de Coordination du CNRS, 205 route de Narbonne 31077 Toulouse, France.
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 alpha-, beta-, and delta-meso positions by a C4-centered radical derived from artemisinin.
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