Three series of aza-artemisinin derivatives were synthesized for studies of anticancer activity. The first series of compounds were prepared via copper(I)-catalyzed azide alkyne cycloaddition, so called "click reaction", starting from propargyl derivatives of 11-aza-artemisinin and various azides, whereas the second and third series of compounds were prepared by triazolization reaction starting from enolizable ketones and primary amines connected to artemisinin. In vitro studies of the 23 synthesized artemisinin derivatives unveiled that 9 compounds displayed antiproliferative activity in the low micromolar range, with 5d being the most promising compound showing 50% inhibition of Cem and HeLa cell growth at 0.92 and 1.2µM, respectively.