Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates
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Date
2023
Journal Title
Journal ISSN
Volume Title
Publisher
Society of Pharmaceutical Sciences of Ankara (FABAD)
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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. © 2023 Society of Pharmaceutical Sciences of Ankara (FABAD). All rights reserved.
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Keywords
1,2,4-Triazole, Cancer, Cox-1/2, Mpges-1, Paracetamol
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Fields of Science
Citation
WoS Q
N/A
Scopus Q
Q4
Source
Fabad Journal of Pharmaceutical Sciences
Volume
48
Issue
3
Start Page
395
End Page
410