WoS İndeksli Yayınlar Koleksiyonu

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

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  • Conference Object
    Comparison of the Effectiveness of Connective Tissue Massage and Classical Massage in Patients with Migraine
    (Elsevier, 2025) Ozdincler, Arzu Razak; Kaya, Begum Kara; Kahleogullari, Elif
  • 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.
  • Conference Object
    Motor Imagery-Based Individualized Alpha Transcranial Alternating Current Stimulation: Effects on Brain Oscillations and Motor Function
    (Elsevier, 2025) Aktuerka, Tuba; Bingol, Elifnur; Bas, Busra; Varolgunes, Yaren; Karadag, Gizem; Unsal, Esra; Guntekin, Bahar
  • Article
    Citation - WoS: 2
    Citation - Scopus: 2
    Novel Triazole-Urea Hybrids as Promising EGFR Inhibitors: Synthesis, Molecular Modeling and Antiproliferative Activity Studies Against Breast Cancer
    (Elsevier, 2025) Ture, Asli; Gulcan, Mehmet Metehan; Birgul, Serap Ipek Dingis; Erdogan, Oguz; Erdogan, Omer; Tuncay, Fulya Oz; Kucukguzel, Ilkay; Öz Tuncay, Fulya; Dingiş Birgül, Serap İpek
    Breast cancer is the second leading cause of mortality among women globally. In this study, novel promising urea derivatives containing a 4-phenyl-5-sulphanylidene-4,5-dihydro-1H-1,2,4-triazole group were synthesized and evaluated for their biological activities against breast cancer. The cytotoxicity and apoptotic profiles of these compounds were assessed on the MCF7 breast cancer cell line and the L929 fibroblast cell line. Compound 5c exhibited the strongest anticancer activity against MCF7 cells with an IC50 value of 56.97+4.22 mu M, while it showed significantly lower cytotoxicity against L929 cells (IC50 = 1651+18.39 mu M). Compound 5c also induced early apoptosis in MCF7 cells, with an apoptosis rate of 18.40% and 5.28%, respectively. Additionally, the EGFR inhibitory activities of the synthesized compounds were evaluated, with compound 5i demonstrating the most potent EGFR inhibition, showing an IC50 value of 35.1 nM. These results suggest that compound 5c likely exerts its anticancer effects through mechanisms other than EGFR inhibition, while compound 5i has significant potential as an effective EGFR inhibitor. Molecular modeling studies were conducted to suggest putative binding interactions of compounds 5d, 5e and 5i with wildtype hEGFR. Further studies are warranted to explore their activity against other cancer types.
  • Article
    Citation - WoS: 10
    Citation - Scopus: 10
    Novel Azole-Urea Hybrids as Vegfr-2 Inhibitors: Synthesis,<i> In</I><i> Vitro</I> Antiproliferative Evaluation And<i> In</I><i> Silico</I> Studies
    (Elsevier, 2023) Shirzad, Mohammad Musa; Kulabas, Necla; Erdogan, Omer; Cevik, Ozge; Dere, Damla; Yelekci, Kemal; Kucukguzel, Ilkay
    The vascular endothelial growth factor receptor-2 (VEGFR-2) is a receptor tyrosine kinase known to be abnormally expressed in various malignant tumors, including breast cancer, and is considered one of the most important contributors to tumor angiogenesis. Sorafenib is one of many VEGFR-2 inhibitors that have received approval for clinical use from the US FDA in recent years. Accordingly, in this study, the synthesis of two new pyrazoles, six 1,3,4-oxadiazoles, four 1,3,4-thiadiazoles, and ten 1,2,4-triazole-3-thione derivatives having structural characteristics similar to sorafenib was carried out. A preliminary screening of synthesized compounds and known inhibitors sorafenib and staurosporine at 10 mu M concentration on in vitro activity of VEGFR-2 was performed, and compounds 10c, 8a, and 11 g were identified as the most potent derivatives with% VEGFR-2 residual activities lower than 30%, and dose-dependent inhibition studies was carried out to determine the IC50 values of these inhibitors. Compound 10c was found to be the most potent inhibitor of VEGFR-2 activity with an IC50 value of 0.664 mu M. The anti-proliferative activity of synthesized derivatives was assessed against a breast carcinoma (MCF-7) cell line, a triple negative human breast adenocarcinoma (MDA-MB-231) cell line, and noncancerous fibroblast cells (L929). Compound 8a displayed superior activity when compared to sorafenib against MCF-7 (7.69 fold) and MDA-MB-231 (1.52 fold) cell lines while displaying 3.75-fold less toxicity against the normal L929 cell line. Annexin V binding assay revealed that compound 8a significantly increased early and late apoptosis in MCF-7 cells and late apoptosis and necrosis in MDA-MB-231 cells. Computational studies such as molecular docking and ADMET evaluation were performed to elucidate the binding interactions and druglikeness of the synthesized compounds. The results indicate that compound 8a could be a promising candidate for the development of a novel anti-angiogenic and anti-proliferative agent.
  • Article
    Citation - WoS: 6
    Citation - Scopus: 6
    Tuning the Magnetic and Magnetocaloric Properties of a Compound Via Mixing (1-X).la0.67ca0.33mno3+x.la0.67sr0.33mno3 (x=0, 0.25, 0.50, 0.75, 1): Composite Materials or Composite Compounds?
    (Elsevier, 2023) Coskum, Atilla; Irmak, Ali Ekber; Altan, Baris; Ak, Yavuz Selim; Coskum, Arictan Tulga; Coşkun, Atilla
    This study aims to optimize the magnetic and magnetocaloric properties of composite materials (or compounds) produced by mixing different ratios of two manganite compounds having different structural, magnetic, and magnetocaloric properties. The parent compounds were prepared using the sol-gel production method and the ultrasonic bath mixing technique was involved to prepare desired composite materials. SEM analyses revealed that the parents and composite materials have the same surface morphologies except for their grain sizes. EDS analyses were performed to identify the possible/candidate phases in the composite materials. These candidate phases are involved in refining XRD data. The fact that the Curie temperatures (TC) of the composite materials were found to be much higher than those of the parent compounds was another proof that composite compounds were obtained instead of composite materials by using the ultrasonic bath mixing technique. Although the TC of the composite compounds was higher than those of the parent compounds, the maximum magnetic entropy values were found to vary between the maximum magnetic entropy valuesof the parent compounds.
  • Article
    Citation - WoS: 13
    <i>in</I><i> Vitro</I> Assessment of Dermatological Activity Potential Of<i> Achillea</I><i> Clypeolata</I> Sm. in H2o2-Treated Human Dermal Fibroblasts
    (Elsevier, 2023) Barak, Timur Hakan; Kurt-Celep, Inci; Dilek-Tepe, Hafize; Bardakci, Hilal; Akaydin, Galip; Yesilada, Erdem; Celep, Engin
    Members of Achilllea L. genus are widely used against dermatological disorders in traditional medicine. An increasing number of experimental studies indicated that these species are an important source of ailments against such conditions. Besides, clinical studies yield supportive results about the dermatological effects of the genus. However, the number of studies stating the mechanisms of actions is quite scarce. A. clypeolata Sn. grows naturally in the Thrace region of Turkiye, and is used against various health problems in folk medicine. The methanolic extract prepared from the aerial parts of the plant (ACM) was subjected to a series of tests focusing on the mechanisms of dermatological activity. First, in vitro antioxidant screening tests, including DPPH, CUPRAC, FRAP and TOAC were applied. Then, the inhibitory potential of ACM against skin-related enzymes such as collagenase, elastase and hyaluronidase was measured. For a more detailed profiling of the activity, human dermal fibroblast cells (HDFs) treated with H2O2 were given varying concentrations of ACM. WST-1 analysis was carried out for the assessment of cell viability, and DCFDA (20,70-dichlorofluorescin diacetate) method was employed for the measurement of cellular antioxidant activity. In addition, the inhibitory potentials of ACM against matrix metalloproteinase-2 and-9 enzymes, which are responsible for the degradation of extracellular matrix components in the skin, were also tested. The total phenolic (26.02 & PLUSMN; 1.04 mg GAE/g dry extract) and flavonoid (12.85 & PLUSMN; 0.69 mg QE/g dry extract) contents of ACM were calculated with the activity tests. Also, for a comprehensive quantitative analysis, LC-MS/MS analysis was carried out. All of the data gained from the mentioned tests and analysis revealed the high capacity of ACM in dermatological conditions such as the inhibitory potential enzymes associated with skin aging. Phytochemical profiling studies showed that the extract is rich in phenolic compounds, specifically chlorogenic acid, hesperidin and hyperoside. Data obtained from this study suggest that A. clypeolata may act as a natural source of skin-active ingredients. & COPY; 2023 SAAB. Published by Elsevier B.V. All rights reserved.
  • Article
    Citation - WoS: 2
    Citation - Scopus: 1
    Synthesis and Investigation of Cytotoxic Effects of Compounds Derived From Flurbiprofen
    (Elsevier, 2023) Gokoglan, Ecem; Dere, Damla; Bedir, Ipek; Yelekci, Kemal; Telci, Dilek; Kucukguzel, S. Guniz
    New flurbiprofen derivatives containing 1,2,4-triazoline-5-thione (4) and thioethers (5a-r) were synthesized in this study. The structures of synthesized compounds were characterized by spectral methods (FT-IR, 1H NMR, 13C NMR) and 19F NMR (only compound 5l), besides elemental analysis. In addition, molecular binding of these compounds to the human methionine aminopeptidase 2 enzyme was performed using AutoDock 4.2, the software product of the research, computationally. All synthesized compounds were evaluated for cytotoxic effect against MDA-MB231 triple-negative breast cancer cell line by using WST-1 Cell Viability and Proliferation assay. Doxorubicin is in the anthracycline class and is an antineoplastic agent. It is used to provide regression in common neoplastic conditions such as breast carcinoma. Due to the cardiovascular side effects of doxorubicin, a combination study was conducted with the (& PLUSMN;)(R,S)-3-{1-[2-fluoro-(1,1 & PRIME;-biphenyl)-4-yl]ethyl}-4-methyl-5-{[2(trifluoromethyl)benzyl]thio}-4H-1,2,4-triazole (5l) with promising cytotoxic effects. As a result of the combination, it was shown as 7% MDA-MB231 cell viability. Therefore, based on the evaluations, a better cytotoxic effect was achieved with the 5l combination depending on the low dose of doxorubicin.
  • 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.
  • Review
    Citation - WoS: 1
    Citation - Scopus: 1
    Effect of Everolimus on Prognosis of Neurofibromatosis Type 1 Lesions: a Systematic Review and Meta Analysis
    (Elsevier, 2024) Ibrahim, Ismail A.; Abdelkader, Rem Ehab; Nada, Ahmed Hosney; Younes, Siham; Hanen, George; Shahwan, Ghena; Nashwan, Abdulqadir J.
    Purpose: This study addresses the effectiveness of oral everolimus in treating various malignancies associated with Neurofibromatosis Type 1 (NF1). The purpose is to determine whether everolimus reduces lesion size in NF1 patients, considering the controversial findings from previous clinical trials. The scientific hypotheses and questions involve evaluating the impact of everolimus on NF1-associated lesions and understanding the variability in treatment outcomes. Methods: A systematic review and meta-analysis were conducted following PRISMA and Cochrane Collaboration guidelines. The study included four-phase II, single-arm, nonrandomized trials investigating the effect of oral everolimus on NF1-associated lesion size. The search covered multiple databases, and data extraction involved evaluating studies for inclusion criteria and assessing quality using the Cochrane Collaboration's Risk of Bias in Nonrandomized Studies tool. Statistical analysis utilized Open Meta(Analyst). Findings: The search yielded 388 studies, with 10 selected for full-text review and four included in the final analysis. The quality of the studies ranged from low to moderate. The meta-analysis indicated no observed heterogeneity (I2 = 0%), and the overall estimate suggested no significant reduction in NF1-associated lesion size with everolimus ( P = 0.069). Implications: The findings reveal a varied and inconsistent picture of everolimus efficacy in NF1 treatment. The study highlights the need for personalized approaches, considering individual genetic and clinical differences. The limitations, including small sample sizes and nonrandomized trials, call for larger, more standardized research efforts. The study emphasizes ongoing trials and the importance of future research in understanding predictors of everolimus response and optimizing treatment strategies for NF1 patients. Conclusion: While everolimus shows promise in reducing lesion size in a subset of NF1 patients, the study cannot draw conclusive results due to limitations in the included studies. Ongoing, adequately powered trials are crucial for advancing the evidence base and informing the potential role of everolimus in NF1 treatment. Others: There was no funding for this review and no conflicts of interest.