Design, synthesis and anticancer activity evaluation of aziridine-1,2,3-triazole hybrid derivatives

Abstract

Abstract New 1-aryl-4-[(aziridine-1-yl)diarylmethyl]-5-methyl-1 H -1,2,3-triazole derivatives 7a–i were synthesized by a one-pot reaction of diaryl-(1-aryl-5-methyl- 1H -1,2,3-triazol-4-yl)methanols 6a–i derived from 1-aryl-5-methyl-1 H -1,2,3-triazole-4-carboxylic acids 4a–c . Structures of compounds 7a–i were confirmed by analysis of proton nuclear magnetic resonance ( 1 H NMR) and carbon-13 nuclear magnetic resonance ( 13 C NMR), mass spectrometry (MS) and infrared (IR) data. The structure of compound 7f was studied by X-ray diffraction analysis. The anticancer activities of compounds 7a–i against human leukemia HL-60 cells and human hepatoma G2 cells were evaluated. Some of the compounds are highly active.