Artemisinin Dimers Derivatives Of Isobutylene-based Bridging Radical Cleavage

Several 1,2,4-trioxane dimers have high in vitro antimalarial, antiproliferative andantitumor activities, and some have high in vivo anticancer activity. Here we preparedtrioxane isobutylene dimer with high activities and stability and carried out cleavagereactions in presence of FeSO₄. Furthermore, we explored the consequence of thepresence of cysteine in which trace iron ion was only needed. We try to explain howand why the dimers of dihydroartemisinin retained the endoperoxide bridges have bothantimalarial and antitumor activity by means of the reaction mechanism. The mode ofaction to cleave the peroxy bond into free radicals maybe explains antimalarial andantitumor activities of the dimer of the dihydroartemisinin from molecules level. Theresult may provide a little support for research of structure-function relation andexploitation of new antimalarial drugs.