Characterization of the Main Radical and Products Resulting from a Reductive Activation of the Antimalarial Arteflene (Ro 42-1611).

The peroxide-containing antimalarial drug arteflene (Ro 42-1611) generates an alkyl radical after the reductive homolytic cleavage of the peroxide bond in the presence of a heme model Mn(II)(TPP). This alkyl radical has been trapped by TEMPO, and the different products of the reduction activation of arteflene have been characterized. These data suggest that, in these experimental conditions, arteflene is not a significant alkylating agent compared to artemisinin, a trioxane-containing antimalarial drug.