Synthesis of novel artemisinin-triazole hybrids

Abstract

Several substituted triazole-artemisinin hybrids were synthesized based on ‘click’ chemistry between propargyl-substituted derivatives and artemisinin containing a 2-hydroxypropane unit. The structures of all obtained compounds were confirmed by means of IR, NMR, and MS spectroscopy. Four new hybrids were evaluated as cytotoxic agents, revealing an interesting anticancer activity of 1-(4-(3-Aminophenyl)-1H-1,2,3-triazol-1-yl)-3-(((3R,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyl-decahydro-12H-3,12-epoxy [1,2] dioxepino [4,3-i] isochromen-10- yl)oxy) propan-2-ol compound in KB and HepG2 cancer cell lines.