TY  - JOUR
TI  - Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates
AB  - 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.
AU  - kulabaş, necla
AU  - GURBOGA, MERVE
AU  - Bingöl Özakpınar, Özlem
AU  - Liu, Jianyang
AU  - Jakobson, Per-Johan
AU  - Danış, Özkan
AU  - Ogan, Ayse
AU  - Küçükgüzel, İlkay
PY  - 2023
JO  - FABAD Journal of Pharmaceutical Sciences
VL  - 48
IS  - 3
SN  - 1300-4182
SP  - 395
EP  - 410
DB  - TRDizin
UR  - http://search/yayin/detay/1209401
ER  -