Design, synthesis and antiproliferative activity of novel phenothiazine-1,2,3-triazole analogues

作者:Ma, Xiao-Hua; Liu, Nan; Lu, Jing-Li; Zhao, Jie; Zhang, Xiao-Jian*
来源:Journal of Chemical Research, 2017, 41(12): 696-698.
DOI:10.3184/174751917X15122516000140

摘要

A series of seven novel 1-aryl-1,2,3-triazole derivatives bearing a 4-(phenothiazin-10-ylmethyl) moiety were designed using a molecular hybridisation approach and synthesised by alkyne/azide click chemistry. Most of the synthesised compounds exhibited moderate to good antiproliferative activity (IC50 values: 0.5 to 6.7 mu M) against stomach, oesophagus, prostate, breast and liver cancer cell lines, but a compound containing a 4-chlorophenyl moiety showed better activity against all cell lines than 5-fluorouracil.