Alkylating Properties of Antimalarial Artemisinin Derivatives and Synthetic Trioxanes when Activated by a Reduced Heme Model

Radicals derived from the antimalarial drug artemisinin (right) were found to be efficient alkylating agents towards the heme model tetraphenylporphyrin after reductive activation of its peroxide function. This reactivity, shared by synthetic analogues of artemisinin, will contribute to the understanding of the in vivo reactivity of artemisinin, and give a better molecular basis for the rational design of new synthetic antimalarial compounds having an epoxide function.