Synthesis and Anticancer Activity of 11-azaartemisinin Derivatives Bearing 1,2,3-triazole Moiety

A series of new compounds were prepared under mild reaction conditions using click reaction of 11-azaartemisinin and various azides. All the synthesized compounds were fully characterized by spectral data and evaluated for their cytotoxic activity against KB and HepG2 cell lines. All synthesized artemisinin derivatives are more active than 11-azaartemisinin. Thirteen of the synthesized compounds displayed good cytotoxic activity against two human cancer cell lines, KB and HepG2, with half maximal inhibitory concentration values in a range of 4.27–70.40 μM. The most active derivative was the best to both KB and HepG2 cell lines with IC50 value of 10.18 and 4.27 μM, respectively.