Yayınlanmış 1 Ocak 2022
| Sürüm v1
Dergi makalesi
Açık
Synthesis and evaluation of antiproliferative and mPGES-1 inhibitory activities of novel carvacrol-triazole conjugates
Yazarlar/Oluşturanlar
- 1. Marmara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34854 Istanbul, Turkey
- 2. Marmara Univ, Fac Pharm, Dept Biochem, TR-34854 Istanbul, Turkey
- 3. Kadir Has Univ, Fac Engn & Nat Sci, Dept Bioinformat & Genet, Istanbul, Turkey
- 4. Marmara Univ, Fac Sci, Dept Chem, TR-34722 Istanbul, Turkey
Açıklama
Some novel triazole-bearing acetamide derivatives 9-26 were synthesized starting from carvacrol. All synthesized compounds were characterized by FTIR,1H-NMR,13C-NMR and MS data. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human chronic myelogenous leukemia K562, human neuroblastoma SH-SY5Y cell lines) were evaluated by MTT assay. Compounds were also tested on mouse embryonic fibroblast cells (NIH/3T3) to determine selectivity. Eighteen target compounds 9-26 were screened for their mPGES-1 and COX-1/2 inhibitory activities. Of these compounds, 26 (KUC16D425) showed the highest mPGES-1 inhibition at 10 mu M. This compound has also been observed to induce apoptosis and inhibit cell migration in MCF-7 cells. In silico molecular docking calculations were performed to understand the binding interactions of compounds with target proteins. ADMET predictions were also done to evaluate drug-like properties of the novel compounds.
Dosyalar
10-25135-acg-oc-142-2212-2651.pdf
Dosyalar
(982.9 kB)
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