Yazar "Uslu H." seçeneğine göre listele

Listeleniyor 1 - 2 / 2
  • Küçük Resim Yok
    Öğe
    (E)-1-(4-Hydroxyphenyl)-3-(substituted-phenyl) prop-2-en-1-ones: Synthesis, in Vitro Cytotoxic Activity and Molecular Docking Studies
    (Slovensko Kemijsko Drustvo, 2022) Sirka L.; Doğan H.; Bahar M.R.; Çalışkan E.; Tekin S.; Uslu H.; Koran K.
    A series of chalcone compounds (2–11) were designed and synthesized to determine their cytotoxic effects. The structures of 2–11 were fully characterized by their physical and spectral data. The in vitro cytotoxic effects of 2–11 were evaluated against human ovarian cancer (A2780), breast cancer (MCF-7) and prostate cancer (PC-3 and LNCaP) cell lines. The activity potentials of compounds were further evaluated through molecular docking studies with AutoDock4 and Vina softwares. All the compounds (except compound 5) showed significant cytotoxic effects at high doses in all cancer cell lines. Among all the compounds studied, one compound i.e. compound 2 demonstrated dose-dependent activity, particularly against A2780/LNCaP cancer cell lines. The most effective compounds 8, 9, 10 and 11 reduced the cell viability of A2780, MCF-7, PC-3 and LNCaP cells by 50–98%, while other compounds 2, 4 and 7 reduced the cell viability of A2780 cells by 70–90% at concentrations of 50 and 100 µM. © 2022 Slovensko Kemijsko Drustvo. All rights reserved.
  • Küçük Resim Yok
    Öğe
    Synthesis and cytotoxicity studies on new pyrazolecontaining oxime ester derivatives
    (University of Benin, 2021) Karakurt A.; Bozbey I.; Uslu H.; Sari S.; Ozdemir Z.; Salva E.
    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.