Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates

Abstract

Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized, and their structures were verified by FTIR, NMR (1H and 13C) and mass spectral data. Compounds 9-20 were tested against five human cancer cell lines (lung cancer A549, chronic myelogenous leukemia K562, breast cancer MCF-7, prostate cancer PC-3, neuroblastoma SH-SY5Y cell lines) for in vitro cytotoxic activities. They were also evaluated their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity by MTT assay. Additionally, we evaluated the potential mPGES-1 and COX-1/2 inhibitory effect of twelve target compounds 9-20. While none of the synthesized compounds exhibited significant inhibition against both cancer cells and mPGES-1 as well as COX-1/2, it was determined that they were not cytotoxic against healthy cells, too. Finally, ADMET properties of newly synthesized compounds were estimated using in silico methods.