WoS İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6
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Article Novel Hydrazide-Hydrazone Derivatives Containing Flurbiprofen 1,2,4-Triazole as Anticancer Agents: Design, Synthesis and Biological Evaluation(Slovensko Kemijsko Drustvo, 2026) Küçükgüzel, Ş. Güziz; Gökoğlan, Ecem; Yılmaz, Özgür; Çevik, Özge; Çakıcı, Çiğdem; Erdoğan, ÖmerHydrazone derivatives are one of the scaffolds frequently used in new drug development studies. Due to the promising pharmacological effects of the hydrazone structure, fifteen new hydrazide-hydrazone compounds containing flurbiprofen 1,2,4-triazole were synthesized in this study and their in vitro anticancer effects were tested. All compounds were tested for cytotoxic effects against breast cancer cell lines (MCF-7 and MDA-MB231), and glioblastoma cell line (U87) by using MTT assay. Among the synthesized compounds, compounds 7a and 7c exhibited the most potent cytotoxic activity with IC50 values of 7.80 +/- 1.20 & micro;M and 2.40 +/- 0.93 & micro;M against MCF-7 cell line, while compound 7a showed the highest activity with IC50 value of 7.63 +/- 1.05 & micro;M against MDA-MB231 cell line. In addition, compounds 7c and 7n presented cytotoxic activity with IC50 values of 10.31 +/- 4.63 & micro;M and 10.81 +/- 6.11 & micro;M against U87 cell line. The possible cytotoxic effects of compounds on mouse fibroblast cell line (L929) were assessed for their safety and compounds 7a, 7c, and 7n were found less toxic than 5-fluorourasil. Additionally, compound 7c was further studied to investigate its effects on apoptosis and PI3K activity, which play a role in cancer development. The results showed that compound 7c increased apoptosis in MCF-7 cells and it displayed PI3K enzyme inhibitory activity. Our study revealed that the synthesized hydrazone compounds have the potential to be lead compounds for further studies on cancer.Article Citation - WoS: 1Citation - Scopus: 1Synthesis, Characterization, and Antimicrobial Evaluation of Some Novel Hydrazinecarbothioamides(Galenos Publishing House, 2025) Güler, Emrah; Dinç, Harika Öykü; Dincel, Efe Doğukan; Güzeldemirci, Nuray Ulusoy; Başoğlu-ünal, Faika; Kuran, Ebru Dıdem; Başoğlu, Faika; Ulusoy Güzeldemirci, NurayObjectives: This study focused on synthesizing and characterizing novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety and evaluating their antimicrobial activity against several bacterial strains. The research aimed to identify key structural features that enhance antimicrobial efficacy through structure-activity relationship analysis and identify the minimum inhibitory concentration (MIC) of the most potent compounds to assess their potential for further development as antimicrobial agents. Materials and Methods: Nine novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety were synthesized by reacting 1,2,4-triazole derivatives with thiosemicarbazide precursors, and the products were characterized using infrared spectroscopy, proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR) spectroscopy, and elemental analysis. The antimicrobial activity of these compounds (5a-i) was tested against Klebsiella pneumoniae (K. pneumoniae), Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, and Pseudomonas aeruginosa (P. aeruginosa), using microdilution, disk diffusion, and broth microdilution methods. Dimethyl sulfoxide was used as a negative control, and Vancomycin and Meropenem were used as positive controls, with all results converted to µM for consistent analysis. Results: The synthesized thiosemicarbazide derivatives (5a-i) were confirmed to be structurally correct through Fourier-transform infrared spectroscopy, 1H-NMR, and 13C-NMR spectroscopy. Among the tested compounds, 5e (4-bromophenyl) and 5g (n-propyl) showed significant antimicrobial activity, with 5g exhibiting the strongest effects against S. aureus and P. aeruginosa. Other derivatives, such as 5b (4-NO2Ph), 5c (4-FPh), and 5d (4-ClPh), showed moderate activity, while no significant activity was observed against K. pneumoniae or E. faecalis. Conclusion: The study successfully synthesized a series of novel thiosemicarbazide derivatives with a 1,2,4-triazole moiety and evaluated their antimicrobial potential. Compounds 5e and 5g exhibited significant antibacterial activity, particularly against S. aureus and P. aeruginosa, with MIC values in the low micromolar range. These findings suggest that the compounds hold promise as potential antimicrobial agents, and further studies should focus on optimizing their efficacy and exploring their mechanism of action.