Synthesis and cytotoxicity studies on new pyrazolecontaining oxime ester derivatives
| العنوان: | Synthesis and cytotoxicity studies on new pyrazolecontaining oxime ester derivatives |
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| المؤلفون: | Suat Sari, Harun Uslu, İrem Bozbey, Emine Şalva, Zeynep Özdemir, Arzu Karakurt |
| المصدر: | Tropical Journal of Pharmaceutical Research. 18:1315-1322 |
| بيانات النشر: | African Journals Online (AJOL), 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | chemistry.chemical_compound, Pharmacokinetics, Chemistry, Cell culture, Toxicity, Pharmaceutical Science, Cytotoxic T cell, Pharmacology (medical), Pyrazole, Oxime, Cytotoxicity, IC50, Combinatorial chemistry |
| الوصف: | Purpose: To synthesize a series of new 1-(2-naphthyl)-2-(1H-pyrazol-1-yl)ethanone oxime ester derivatives (5-12) with potential anticancer properties, and to determine their cytotoxic effects in mouse fibroblast and human neuroblastoma cell lines. Methods: The title compounds were obtained through sodium salt reaction of 1-(naphthalene-2-yl)-2- (1H-pyrazol-1-yl)etanone oxime (4) with various acyl chlorides. The cytotoxic effects were evaluated by MTS colorimetric assay, while physicochemical descriptors were calculated using QikProp software. Results: Most of the compounds showed approximately 50 – 60 % inhibition against SH-SY5Y neuroblastoma cells at 100 μM. Of these, compound 7a was the most active combination with an IC50 value of 85.94 µM. The toxic effect of the compounds on mouse fibroblast cell line was insignificant (p < 0.05) even when the dose was increased. The calculated physicochemical properties of the compounds were within drug-like chemical space. Conclusion: The synthesized oxime ester derivatives with pyrazole ring exhibit selective toxicity to neuroblastoma cells without affecting healthy mouse fibroblast cells. The compounds proved to be druglike while their pharmacokinetic features were also encouraging, and were in line with in silico predictions. |
| تدمد: | 1596-9827 1596-5996 |
| DOI: | 10.4314/tjpr.v18i6.24 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::09e5ed9579c547a00009b33d5dd7caf5 https://doi.org/10.4314/tjpr.v18i6.24 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi...........09e5ed9579c547a00009b33d5dd7caf5 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15969827 15965996 |
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| DOI: | 10.4314/tjpr.v18i6.24 |