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

作者：Dong, Hong-Ru^*; Wu, Jian-Guo; Gao, Zhong-Lian

来源：Synthetic Communications, 2017, 47(19): 1783-1796.

DOI：10.1080/00397911.2017.1353632

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

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 H-1 and C-13 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 H-1-NMR signals of the aziridine-ring cis-H/trans-H protons were found to be two group peaks at 1.800-1.884 and 1.183-1.327ppm. @@@ [GRAPHICS] @@@ .

• 出版日期2017
• 单位兰州大学