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Yayın Synthesis of new piperazine‐oxadiazole derivatives and investigation of their anticancer activities(Elsevier, 2025) Uslu, Harun; Göktaş, Bünyamin; Osmaniye, Derya; Levent, Serkan; Peçe Göktaş, Sare; Sağlık Özkan, Begüm Nurpelin; Özkay, Yusuf; Benkli, KadriyeSince cancer is one of the leading causes of human death, recent research has largely focused on developing multi-target drug designs. In this study, we designed and synthesized a series of piperazine-oxadiazole derivatives as aromatase inhibitors for the treatment of cancer. Their structures were confirmed by 1 C NMR, HRMS and FTIR spectroscopic methods. Cytotoxicity (MTT) was performed to determine the anticancer activity of the compounds as aromatase inhibitors against breast (MCF7), fibroblast (NIH3T3) and lung (A549) cell lines. Letrazol was used as the reference agent, compound 4b exhibited a significant effect among other derivatives with a value of IC H NMR, 50 =2.103±0.088 μ 13 Magainst the MCF7 cell line. Docking study showed that 4b was one of the compounds with the best pose on the aromatase. The docking study showed that 4e was one of the compounds that gave the best pose on EGFR and topoisomerase. When the aromatase, EGFR and topoisomerase docking results were compared, it was concluded that our synthesized compounds may be more effective on the Aromatase macromolecule. From the obtained evaluations of the designed batches, compound 4b appeared to be a promising agent as an aromatase inhibitor for further research and evaluation studies in the future.Yayın Synthesis, cytotoxic activity evaluation and molecular docking studies of some benzimidazole derivatives(Sivas Cumhuriyet University, 2024) Kaya, Aybüke Züleyha; Osmaniye, Derya; Evren, Asaf Evrim; Yurttaş, Leyla; Demirayak, ŞerefIn this study, the synthesis of 2-(2-acetyl-1H-benzimidazol-1-yl)-1-arylethanone (3a-3d) and 1-methyl-3-phenylbenzo[4,5]imidazo[1,2-a]pyrazine derivatives (4a-4d) and to investigate their cytotoxic activity were aimed. APCI, IR, 1HNMR, and 13CNMR spectra were utilized to determine the structure of the synthesized compounds. The cytotoxic activity of selected compounds were detected in A549 (human lung carcinoma) and NIH3T3 (mouse embryonic fibroblasts) cell lines. Compounds 4c and 4d were found to be selectively cytotoxic against A549 and NIH3T3 cell lines. Molecular docking studies were performed using the data retrieved from the Protein Data Bank server (PDBID: 4QTX).Yayın A new approach to oral dosage forms: carrageenan-based vegan gummies(Marmara University Press, 2024) Gültekin, Hazal Ezgi; İlhan, Miray; Nalbantoğlu, FıratAlthough the oral route is a common drug administration route, it still causes some patient compliance problems. Gummies are chewable gels that are commonly manufactured as dietary supplement carriers and their pharmaceutical use is still limited. Dexketoprofen trometamol is an anti-inflammatory and antipyretic drug. In the present study, dexketoprofen containing gummies were manufactured using carrageenan (Gelcarin®GP-379) as the gel-forming polymer. Potassium dihydrogen phosphate (KH2PO4) was used as the gelling agent in the research. The obtained gummies were characterized. For this purpose, gel viscosity measurements, morphological and physical characterizations, thermal analysis, and in vitro drug release studies were carried out. The viscosity of the gel mixtures was measured at 50°C, which was the pouring temperature of the gels into molds. The formulation containing the highest carrageenan and KH2PO4 had the highest viscosity. The physical characterization results showed that the gummy formulations could be prepared in a reproducible manner. The DSC thermograms showed that the melting peak of DXT was not observed in the gummy formulation. The in vitro dissolution test results of the gummies showed that decreasing the carrageenan and KH2PO4 concentration in gummy formulation accelerated the drug release. The obtained gummies exhibited an extended-release of up to 2 hours.
