Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates


kulabaş n., GURBOGA M., Bingöl Özakpınar Ö., Liu J., Jakobson P., Danış Ö., ...More

FABAD Journal of Pharmaceutical Sciences, vol.48, no.3, pp.395-410, 2023 (Scopus) identifier

  • Publication Type: Article / Article
  • Volume: 48 Issue: 3
  • Publication Date: 2023
  • Journal Name: FABAD Journal of Pharmaceutical Sciences
  • Journal Indexes: Scopus, EMBASE, International Pharmaceutical Abstracts, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.395-410
  • Marmara University Affiliated: Yes

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.