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    Cytotoxicity effects and biochemical investigation of novel tetrakis-phthalocyanines bearing 2-thiocytosine moieties with molecular docking studies
    (Elsevier, 2022) Günsel, Armağan; Yıldırım, Aslı; Taslimi, Parham; Erden, Yavuz; Taşkın-Tok, Tuğba
    In this study, the novel 3-(4-aminopyrimidin-2-ylthio) phthalonitrile (1) as starting material was synthesized and its molecular structure was verified by the experiment of single crystal X-ray diffraction, and it was first brought to the literature. Then, its non-peripherally tetra-substituted phthalocyanines (2,3) and the methylated derivatives (2a,3a) containing cytosine derivative were synthesized herein for the first time. All the compounds used were characterized with various spectroscopic methods such as UV–Vis, FT-IR, 1H NMR, 13C NMR and MALDI-TOF MS by obtaining highly satisfactory results. The acetylcholinesterase inhibitor compounds recorded as important therapeutic drugs for the therapy of Alzheimer's disease. So, these novel phthalocyanines effectively inhibited acetylcholinesterase enzyme, with Ki values in the range of 31.75 ± 5.72 to 107.15 ± 12.67 µM. For this enzyme, IC50 values were obtained in the range of 3.41 ± 0.78 to 10.08 ± 2.65 µM. For ?-glycosidase enzyme, the most effective Ki values of (3) and (3a) were found as 3.41 ± 0.78 and 5.32 ± 1.34 µM, respectively. We used 50 µL substrates for the acetylcholine esterase and ?-glycosidase enzymes and 20 µL enzymes. For AChE, we used distilled water and buffer 800 µL and 100 µL, respectively. Also, we pipetted 500 µL and 300 µL for ?-glycosidase and examined the activities. Indeed, the most potent phthalocyanines against both enzymes were recorded for the purpose to investigate interaction modes of these compounds in the active site of the target enzyme. After treatment of compounds, viability was reduced by approximately 25% in cancer cell lines. The cytotoxicity potential of these phthalocyanines against human breast, colon, and prostate cancers demonstrated that these compounds had normal cytotoxic effects. © 2022 Elsevier B.V.
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    Novel tetrakis-phthalocyanines bearing pyrimidine derivative: crystal XRD analysis, enzyme inhibition, molecular docking, and anticancer effects
    (Taylor & Francis Online, 2021) Günsel, Armağan; Yazar, Bilge; Taslimi, Parham; Erden, Yavuz; Taşkın-Tok, Tuğba; Pişkin, Hasan
    In this study, the novel 4-(4-Aminopyrimidin-2-ylthio) phthalonitrile (1) as starting material was synthesized and its 3D structure was verified by the single crystal X-ray diffraction experiment. Then, its peripherally tetra-substituted phthalocyanines (2,3) and the methylated derivatives (2a,3a) containing pyrimidine derivative were synthesized. All these newly synthesized compounds were characterized with various spectroscopic methods such as UV-Vis, FT-IR, 1H-NMR, 13C-NMR and MALDI-TOF MS by obtaining satisfactory results. In addition, these novel phthalocyanines effectively inhibited acetylcholinesterase enzyme, with Ki values in the range of 10.43 ± 2.38 to 41.70 ± 9.32 µM. For the related enzyme, the IC50 values were obtained in the range of 11.68 to 44.28 µM. For ?-glycosidase enzyme the most effective Ki values of (3a) and (2) were with Ki values of 92.87 ± 10.70 and 95.18 ± 17.83 µM, respectively. Indeed, the most potent phthalocyanines against both enzymes were recorded for the purpose of investigating interaction modes of these complexes in the active site of the target enzyme. The cytotoxicity potential of these phthalocyanines against human breast, colon, and prostate cancers demonstrated that these compounds had normal cytotoxic effects.Communicated by Ramaswamy H. Sarma.