Synthesis and cytotoxicity studies on new pyrazolecontaining oxime ester derivatives
Küçük Resim Yok
Tarih
2021
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
University of Benin
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
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 ?M. Of these, compound 7a was the most active combination with an IC50 value of 85.94 ?M. 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. © 2019 The authors.
Açıklama
Anahtar Kelimeler
Cytotoxic activity, E/Z isomer, Neuroblastoma cell, Oxime ester, Pyrazole
Kaynak
Tropical Journal of Pharmaceutical Research
WoS Q Değeri
Scopus Q Değeri
Q3
Cilt
18
Sayı
6
