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

ABSTRACT

Some new 1-aryl-4-[(aziridine-1-yl)diaryl-methyl]-5-methyl-1H-1,2,3-triazole derivatives 7j–s were synthesized by the one-pot reaction of diaryl-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)methanol compounds 6j–s formed from 1-aryl-5-methyl-1H-1,2,3-triazole-4-carboxylic acid derivatives. The new compounds 7j–s and 6j–s are investigated by ¹H and ¹³C NMR, MS, and IR. The anticancer activity of the synthesis target compounds was evaluated against human leukemia (HL-60) cells and human hepatoma G2 cells. Some of the compounds were highly efficient. The ¹H-NMR signals of the aziridine-ring cis-H/trans-H protons were found to be two group peaks at 1.800–1.884 and 1.183–1.327 ppm.

GRAPHICAL ABSTRACT

KEYWORDS:

• 1H-1,2,3-triazole
• anticancer
• aziridine
• human hepatoma G2
• human leukaemia (HL-60)
• synthesis

Acknowledgments

The authors wish to acknowledge the funding support by the education department in Gansu province (2016B-124) and by the Lanzhou University of Arts and Science (High levels of achievement projects 2015GSP05).