Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates

Authors : Necla Kulabaş, Merve Gürboğa, Özlem Bingöl Özakpinar, Jianyang Liu, Perjohan Jakobsson, Özkan Daniş, Ayşe Ogan, Ilkay Küçükgüzel

Pages : 395-410

Doi:10.55262/fabadeczacilik.1336831

View : 89 | Download : 126

Publication Date : 2023-10-18

Article Type : Research Paper

Abstract :Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized and their structure were characterized by FTIR, 1H-NMR, 13C-NMR and MS data. In vitro cytotoxic activities of all synthesized molecules against five cancer cell lines (human lung cancer A549, human chronic myelogenous leukemia K562, human breast cancer MCF-7, human prostate cancer PC-3, human neuroblastoma SH-SY5Y cell lines) were examined and were also tested their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity. MTT assay were used these in vitro activity studies. Additionally, twelve target compounds 9-20 were screened for their mPGES-1 and COX-1/2 inhibitory activities. While none of the synthesized compounds showed a 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 data were presented by predicting the drug-like properties of newly synthesized compounds using computational methods.
Keywords : parasetamol, 1, 2, 4 triazol, kanser, mPGES 1, COX 1 2