Sürdürülebilir Kalkınma Amaçları
Yayınlar
- MakaleAçık Erişim2026Scopus SJRQ2Synthesis and pharmacokinetic profiling of a novel pyrimidine imidazole based thiosemicarbazone derivative for BRAF inhibition in lung cancer therapy
Ekincioğlu, Yavuz; Kızıl, Hamit Emre; Güllü, Eda; Özkan, Elvan Hasanoğlu; Nartop, Dilek
This study presents the design, synthesis, and comprehensive evaluation of a novel thiosemicarbazone derivative containing a pyrimidine-imidazole (C11H11N8SCl) as a potential BRAF inhibitor for the treatment of non-small cell lung cancer. The compound was synthesized by a condensation reaction and characterized by elemental analysis, molar conductivity, SEM-EDS, FT-IR, 1H, and 13C-NMR spectral techniques. DFT calculations at the B3LYP/6-311 + + G(d, p) level revealed a HOMO-LUMO gap of 2.8 eV, indicating appropriate molecular stability and reactivity. Molecular docking studies with BRAF (PDB ID: 1UWH) demonstrated favorable binding affinity (-6.85 kcal/mol) with key interactions at ILE512, HIS509, HIS584, GLN529, GLU585, LYS590, VAL510, and LEU587 residues. In vitro cytotoxicity assays revealed that the compound possesses anticancer potential against H-460 cells, with a significant inhibitory effect observed at a concentration of 200 µg/mL. Combined with its favorable binding affinity toward BRAF kinase, these results suggest that the pyrimidine-imidazole thiosemicarbazone may serve as a potential lead scaffold for further development in targeted lung cancer therapy.ADME profiling confirmed the compound’s compliance with Lipinski’s rule of five parameters, supporting its potential as an orally active drug candidate. These findings suggest that our pyrimidine-imidazole thiosemicarbazone represents a promising scaffold for the development of targeted BRAF inhibitors for lung cancer therapy.
- MakaleAçık Erişim2026Scopus SJRQ1Shape-Directed Hydrothermal Design of Zinc Oxide Nanoparticles for Antimicrobial and Anticancer Applications
Özkan, Elvan Hasanoğlu; Yetim, Nurdan Kurnaz; Kızıl, Hamit E.; Öğütçü, Hatice
The emergence of antibiotic-resistant bacteria represents one of the most pressing challenges in global healthcare. In this study, metal oxide–based nanomaterials are gaining prominence due to their antimicrobial and anticancer potential. In the present study, six new zinc oxide nanoparticles (ZnO-NPs) synthesized via the hydrothermal method using different surfactants were characterized, and their biological activities were evaluated. ZnO-NPs, whose structural properties were determined by a range of analytical methods including BET, FT-IR, SEM-EDX, XRD, and XPS, exhibited significant antibacterial and antifungal effects on a range of bacterial and fungal strains. The study revealed that variations in the morphology and surface area had a direct impact on antimicrobial efficacy. In antimicrobial assays, the inhibition zones ranged from 10.5 mm to 25.5 mm, with ZnO-6 exhibiting the highest efficacy against S. epidermidis (25.5 mm). In cytotoxicity assays, ZnO-6 demonstrated the strongest anticancer potential against H460 cells with the lowest IC50 value of 31.9 µg/mL. Furthermore, a strong correlation was revealed between the physicochemical properties of ZnO-NPs and their anticancer activity, as evidenced by the results of tests conducted on H460 lung cancer cells. Specifically, ZnO-6, which possesses a flower-like morphology and the highest surface area, exhibited the strongest anticancer effect with an IC50 value of 31.9 µg/mL. The parallel enhancement in both antimicrobial and anticancer activities observed in ZnO-6 suggests a common underlying mechanism, likely driven by the high surface area and specific flower-like morphology that facilitates increased interaction with cell membranes and ROS generation. The findings demonstrate that the controlled design of ZnO-NPs in terms of morphology and surface area offers significant potential in both antimicrobial and anticancer applications.
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İncele - MakaleAçık Erişim2020Asimetrik Schiff Bazı Ni(II) Komplekslerinin Antimutajenik Aktivitesinin Değerlendirilmesi
Nartop, Dilek; Özkan, Elvan Hasanoğlu; Kizil, Hamit Emre; Agar, Guleray; Sarı, Nurşen
Bu çalışmada, asimetrik Ni(II) kompleksleri (NiL1, NiL2, NiL3, NiL4) potansiyel antimutajen özelliklerini incelemek için son zamanlarda grubumuzdan biri tarafından rapor edilen yeni iki aşamalı bir yöntem ile hazırlandı. Lenfositlerdeki sodyum azid kaynaklı antimutagenik etki, kardeş kromatid değişimi (SCE) ve mikronükleus (MN) yöntemleriyle belirlendi. Sentezlenen bileşiklerin antimutagenik özelliklere sahip olduğu ve pozitif kontrol olarak kullanılan sodyum azid (NaN3) 'ün neden olduğu mutajeniteyi azalttıkları belirlenmiştir.
AtıfOpenAlex3
İncele - MakaleAçık Erişim2020Synthesis of novel polymers containing Schiff base as potential antimutagenic and antimicrobial agents
Nartop, Dilek; Tokmak, Erkan; Özkan, Elvan Hasanoğlu; Kızıl, Hamit Emre; Öğütcü, Hatice; Ağar, Güleray; Allı, Sema
In this research study, two novel polymers including Schiff base were prepared by condensation reaction of polystyrene-A-NH2 with 5-nitro-2-thiophenecarboxaldehyde/or 5-(2-nitrophenyl)-2-furancarboxaldehyde. The synthesized polymers were evaluated using the elemental analysis, infrared spectroscopy (IR), gel permeation chromatography (GPC), thermal gravimetric analysis (TG/DTA). In addition, the antimicrobial and antimutagenic study of the polymers were reported. The antibacterial and antifungal activity were investigated using the diffusion method against pathogenic bacterial strains. PA-TC and PA-FC polymers exhibited the highest antimicrobial activity against the S. typhi H. and P. vulgaris, respectively. PA-FC polymer revealed the highest antifungal activity against C. albicans. The antimutagenic effects were evaluated using the sister chromatid exchange (SCE) and micronucleus (MN) methods against the sodium azide (NaN3) in human lymphocyte cells. The results demonstrated that the PA-FC polymer have strong antimutagenic properties, especially in the concentration of 20 µg/mL.
AtıfScopus10OpenAlex2İncele