WoS İndeksli Yayınlar Koleksiyonu

Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6

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  • Article
    New Diclofenac Hydrazones: Design, Synthesis, in Silico Studies and Anticancer Evaluation Against Breast Cancer
    (Elsevier, 2026) Birgul, Kaan; Oktay, Lalehan; Bekci, Hatice; Cikla-Suzgun, Pelin; Durdagi, Serdar; Kucukguzel, S. Guniz
    Breast cancer remains one of the most prevalent and lethal malignancies among women, highlighting the urgent need for novel therapeutic strategies that can overcome resistance mechanisms. The p38 alpha mitogen-activated protein kinase (MAPK14) plays a key role in inflammation-associated oncogenic signaling, making it an attractive molecular target for drug development. In this study, a novel series of diclofenac-based hydrazone derivatives (4a-4o) were designed, synthesized, and characterized using FT-IR, 1H- and 13C-NMR spectroscopy, thin-layer chromatography, and elemental analysis. Computational target profiling using SwissTargetPrediction identified MAPK14 as the primary predicted target. Molecular docking against the MAPK14 crystal structure (PDB ID: 1WBS) revealed high binding affinities (-11.41 to -8.34 kcal/mol), supported by MM/GBSA free energy calculations and molecular dynamics simulations, which confirmed stable ligand-protein interactions through hydrogen bonding with Asp168 and Glu71. In vitro cytotoxicity assays on MCF-7 (luminal A) and MDA-MB-231 (triple-negative) breast cancer cell lines demonstrated low-micromolar IC50 values, with compounds 4c, 4d, and 4e showing the strongest activity (2.1-4.5 mu M), surpassing the reference drug Tamoxifen. Overall, the results indicate that diclofenac hydrazones represent promising candidates anticancer properties through MAPK14 inhibition, providing a foundation for the development of next-generation therapeutics against breast cancer.
  • Article
    Citation - WoS: 1
    Neuroprotective Effect Of<i> Myrtus</I><i> Communis</I> Against Ionizing Radiation-Induced Brain Injury: Insights From Histopathological and Biochemical Analysis in Rats
    (Elsevier, 2024) Aslan, Dicle; Alan, Burcu; Yay, Nagehan Ozyilmaz; Karaoglu, Sumeyye Yilmaz; Ertas, Buesrara; Sen, Ali; Atasoy, Beste M.
    Aim: To investigate the potential radioprotective effects of Myrtus communis on brain tissue. Methods: Thirty female rats were divided into four groups. The control group (C) was applied with oral saline solution (SF) for four days. Myrtus communis (MC) groups started to receive MC (100 mg/kg, oral) either four days before (R + preMC) or immediately after (R + MC) irradiation for four days. Irradiation was applied 10 Gy in a single fraction. All rats were sacrificed on the fourth day of irradiation. Malondialdehyde (MDA), nitric oxide (NO), and glutathione (GSH) levels, myeloperoxidase (MPO), superoxide dismutase (SOD), and tissue factor activities (TFa) were determined for biochemical analysis. Hematoxylin&Eosin &Eosin staining was done for histopathological analyses, and electrophoretic analyses were performed. Results: NO, MDA, and MPO levels were higher in all irradiated groups compared with the C group. MC administration decreased NO, MDA, and MPO levels in R + preMC and R + MC groups. MC administration increased GSH levels. TFa activity decreased in R groups but did not change with MC administration compared to the C group. Radiation-induced brain tissue injury decreased, and morphologically normal neurons were observed in both MC-added groups. Conclusion: Myrtus communis has a potential neuroprotective effect on brain tissue, attributed to its antioxidative, anti-inflammatory, and anti-lipid peroxidative properties.