Browsing by Author "Jakobsson, P.-J."

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Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates
(Society of Pharmaceutical Sciences of Ankara (FABAD), 2023) Kulabaş, N.; Gürboǧa, M.; Özakpinar, Ö.B.; Liu, J.; Jakobsson, P.-J.; Daniş, Ö.; Küçükgüzel, I.
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.