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    Imidazole-Derived Alkyl and Aryl Ethers: Synthesis, Characterization, In Vitro Anticancer and Antioxidant Activities, Carbonic Anhydrase I-II Inhibition Properties, and In Silico Studies
    (Amer Chemical Soc, 2024) Faris, Mays; Bostanci, Hayrani Eren; Ozcan, Ibrahim; Ozturk, Mustafa; Kocyigit, Umit Muhammed; Erdogan, Taner; Tahtaci, Hakan
    Imidazole derivatives display extensive applications in pharmaceutical chemistry and have been investigated as bioactive compounds for medicinal chemistry. In this study, besides the starting materials (3a-c and 4a-c), synthesis, characterization, and biological activity studies were conducted on a total of 18 compounds, nine of which are known and the other nine are original. The compounds investigated in the study are a series of alkyl (7-15) and aryl (16-24) ether derivatives bearing substituted phenyl and imidazole rings, which were characterized using various methods including H-1 NMR, C-13 NMR, FT-IR analysis, elemental analysis, and mass spectroscopy. Computer-aided drug design studies have been carried out to predict the biological activities of compounds. Besides DFT calculations, the binding affinities of the compounds to EGFR, VEGFR2, FGFR1, HSP90, hCA I, and hCA II were investigated. Additionally, drug-likeness and ADME analyses were performed on the compounds. Anticancer, antioxidant, and enzyme inhibition activity tests were performed in biological activity studies on the synthesized compounds. Among the synthesized compounds, compounds 17 and 19-24 generally exhibited inhibition profiles against the widespread cytosolic hCA I isozyme with IC50 values ranging from 4.13 to 15.67 nM and cytosolic hCA II isozyme with IC50 values ranging from 5.65 to 14.84 nM. L929 (mouse fibroblast cell line) was used as the control healthy cell line, and MCF7 (breast cancer), C6 (rat glioblastoma), and HT-29 (colon cancer) cells were used in cell culture studies as cancer cell lines. Before the study on cancer cells, all compounds were examined on healthy cells, and their cytotoxicity was determined. As a result of these data, studies continued with six compounds determined to be nontoxic. On cancerous cells, it was determined that compounds 3a, 3b, 4a, 4b, 4c, and 7 had cytotoxic effects on both colon cancer and brain tumors. It was found that compound 3b had a more toxic effect than cisplatin on the glioma cell line with an IC50 value of 10.721 +/- 0.38 mu M, and compound 3a had a more toxic effect on the colon cancer cell line with an IC50 value of 20.88 +/- 1.02 mu M. However, it was determined that the same compounds did not have a statistically significant effect on breast cancer. Flow cytometry studies also showed that when the IC50 dose of compound 3b was applied to the C6 cell line, the cells tended to early and late apoptosis. Additionally, it has been shown by flow cytometry that the cell cycle stops in the G0/G1 phase. A similar effect was observed in the colon cancer cell line with compound 3a. Compound 3b caused early and late apoptosis of the colon cancer cell line with the applied IC50 dose and stopped the cell cycle in the G0/G1 phase. Finally, the FRAP method studied all synthesized compounds' antioxidant effects. According to the measured antioxidant power results, it was determined that no compound had a more effective reducing power than vitamin E.
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    Synthesis and Characterization of Oxime Derivatives and their Some Transition Metal Complexes with Thiadiazole Groups: Biological Activities, and Molecular Docking Studies of the Ligands
    (Wiley-V C H Verlag Gmbh, 2024) Otaiwi, Ahmed Saleem; Mirghani, Ahmed Hamdi; Bostanci, Hayrani Eren; Coskun, Ahmet; Tahtaci, Hakan; Uysal, Saban
    This study involved the synthesis and investigation of the anticancer and antioxidant capabilities of six newly developed ligands generated from 1,3,4-thiadiazole and diphenyl ether keto oxime which has never been synthesized before, together with their transition metal complexes. The obtained ligands were characterized using elemental analysis, FTIR, 1H NMR, 13C NMR, and mass spectroscopy. Polymeric complexes of the obtained ligands were synthesized by reacting all ligands with MCl2.nH2O (M: Mn2+/Co2+)/Ni2+/Cu2+)) salts. The polymeric complexes ' structures were determined using elemental analysis, ICP-AES, FTIR spectroscopy, UV-vis spectroscopy, magnetic susceptibility analysis, and thermogravimetric analysis. Subsequently, the ligands were examined for their anticancer properties. To achieve this objective, the HT-22 cell line, which consists of healthy mouse hippocampus neuronal cells, is utilized as the control group. Additionally, the MCF7 (breast cancer), MDA-MB-231 (breast cancer), C6 (rat glioma), HT-29 (colon cancer), and A549 (lung carcinoma) cell lines are employed in cell culture research as representatives of cancerous cell lines. Based on the cell culture investigations, some of the synthesized ligands showed moderate to good anti-cancer activity, especially for both colon cancer and brain tumors. Finally, a molecular docking analysis was conducted utilizing MOE software to ascertain the binding affinity between the synthesized ligands and the specific proteins of interest. This study includes the synthesis of transition metal complexes of six new ligands obtained from 1,3,4-thiadiazole and diphenyl ether keto oxime and the investigation of the anticancer and antioxidant properties of the ligands. Finally, a molecular docking analysis was performed to determine the binding affinity between the synthesized ligands and specific proteins of interest. image