Synthesis and cytotoxicity of artemisinin derivatives containing cyanoarylmethyl group.

Abstract A series of 12α-deoxoartemisinyl cyanoarylmethyl dicarboxylates ( 4a – 4o ), dicarboxylic acids 12α-deoxoartemisinyl ester cyanoarylmethyl amide ( 5a – 5k ), and dicarboxylic acids 12α-deoxoartemisinyl ester N -methylcyanoarylmethyl amide ( 6a – 6l ), showing moderate cytotoxicity against P388 and L1210 cells were prepared. They induced the significant accumulation of L1210 and P388 cells in the G1 phase of the cell cycle. This mechanism of action was quite different from that of the majority of cytotoxic compounds used in the chemotherapy of cancer. Compound 4b possessed better cytotoxicity than the other compounds.