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: 6Citation - Scopus: 6Synthesis, Antimicrobial Properties and <i>in Silico</I> Studies of Aryloxyacetic Acid Derivatives With Hydrazone or Thiazolidine-4 Scaffold(Taylor & Francis inc, 2023) Senkardes, Sevil; Kart, Didem; Bebek, Bilge; Gunduz, Miyase Gozde; Kucukguzel, S. GunizIn this work, twenty hydrazide-hydrazone and 4-thiazolidinone derivatives were synthesized starting from m-cresol. Antimicrobial evaluation was carried out by microdilution method against Enterococcus faecalis and Staphylococcus aureus as Gram-positive bacteria and Escherichia coli and Pseudomonas aeruginosa as Gram-negative bacteria, and three pathogenic fungi Candida albicans, Candida parapsilosis and Candida krusei. Some compounds possessed considerable antimicrobial properties against the tested microorganisms, particularly against E. coli. 4-Thiazolidinones containing 3-methoxyphenyl and 3,5-dichlorophenyl moieties (4h and 4i) were found to be the most active derivatives with MICs of 2 mu g/mL against E. coli. N'-[(3,5-dichlorophenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide (3i) also displayed antifungal activity against Candida krusei that was comparable to fluconazole. Calculated drug-likeness and ADMET parameters of the most active compounds confirmed their potential as antimicrobial drug candidates. Molecular docking investigations were carried out in the thiamine diphosphate-binding site of pyruvate dehydrogenase multienzyme complex E1 component (PDHc-E1) to clarify the potential antibacterial mechanism against E. coli. The results showed the potential and importance of developing new hydrazones and 4-thiazolidinones that would be effective against microbial strains. Communicated by Ramaswamy H. Sarma