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    Biological activity and molecular docking studies of some new quinolines as potent anticancer agents
    (Humana Press Inc, 2021) Köprülü, Tuğba Kul; Ökten, Salih; Atalay, Vildan Enisoglu; Tekin, Şaban; Çakmak, Osman
    The objective of this study is to investigate the antiproliferative and cytotoxic properties and the action mechanism of substituted quinoline and tetrahydroquinolines 3, 4, 5, 7, and 8 against rat glioblastoma (C6), human cervical cancer (HeLa), human adenocarcinoma (HT29) cancer cell lines by BrdU Cell Proliferation ELISA, Lactate Dehydrogenase, DNA laddering and Topoisomerase I assays. The results of the study showed that 6,8-dibromotetrahydroquinoline 3 possess in vitro antiproliferative activity against C6, HeLa, and HT29 cell lines while morpholine/piperazine substituted quinoline 7 and 8 showed selective antiproliferative activity on C6 cell line with IC50 values 47.5 and 46.3 mu g/mL, respectively. Moreover, 6,8-dibromoTHQ 3 caused DNA fragmentation while it did not inhibit the Topoisomerase I (Topo I) enzyme. On the other hand, compound 8 did not cause DNA laddering while 8 inhibited the Topo I enzyme. According to these results, 6,8-dibromoTHQ 3 stimulates apoptosis on the C6 cell line while 6,8-dibromo-3-morhonilylquinoline (8) inhibits the Topo I enzyme to cause antiproliferative activity. Graphic abstract
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    Functionalized methoxy quinoline derivatives: Experimental and in silico evaluation as new antiepileptic, anti-Alzheimer, antibacterial and antifungal drug candidates
    (Elsevier, 2024) Ciftci, Bilge; Okten, Salih; Kocyigite, Umit Muhammet; Atalay, Vildan Enisoglu; Atas, Mehmet; Cakmak, Osman
    The objective of this study was to assess the inhibitory effects of newly synthesized quinoline derivatives on human carbonic anhydrase I and II (hCA I and II), as well as acetylcholinesterase (AChE) enzymes, alongside their impact on various microorganisms. The synthesized compounds were assessed using IC50, Ki and MIC values via Ellman and Esterease Method and Microdilution assay. Most compounds exhibited strong inhibitory effects on human carbonic anhydrase I and II (hCA I and II) and acetylcholinesterase (AChE), notably compounds 9, 12, and 17 for hCA I, and 9, 12, 16 and 17 for hCA II, alongside robust AChE inhibition by compounds 8 and 13. Antimicrobial tests highlighted compounds 13 and 15 as promising inhibitors against pathogens, particularly effective across various strains. Molecular docking supported these findings, indicating potent binding abilities, notably by compounds 16 and 17 across specific protein structures (2COP, 5E2M, and 6KM3). The discussion emphasized the impact of substituents, particularly methoxy groups at specific positions, on enzyme inhibition, revealing how structural modifications affected enzyme inhibitory properties. The comprehensive analysis bridged experimental and computational findings, uncovering essential structure-activity relationships in quinoline derivatives and identifying potential candidates for further studies in enzyme inhibition and antimicrobial research.
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    Synthesis and spectral properties of symmetrically arylated BODIPY dyes: Experimental and computational approach
    (Elsevier, 2023) Yilmaz, Rasit Fikret; Derin, Yavuz; Misir, Busra Albayrak; Atalay, Vildan Enisoglu; Tutar, Omer Faruk; Okten, Salih; Tutar, Ahmet
    In this study, a series of symmetrically arylated BODIPY dyes were synthesized using a pre-functionalization method, and their structures were characterized by several spectroscopic methods. The relationship between the aryl substitution pattern and the photophysical and electrochemical properties of the dyes was investigated using experimental and computational methods. It was found that electron-donating & pi;-conjugated groups at the meso position and electron-accepting & pi;-conjugated groups at the C3/C5 position led to blue-shifted spectra, while the opposite substitution pattern resulted in red-shifted spectra. Additionally, inductive electron-donating alkyl groups at the meso position produced a blue spectral shift and an alkyl group at the meso position significantly increased the fluorescence quantum yield compared to the arylated counterparts. Computational investigations revealed that a thioanisyl group at the C3/C5 position resulted in a significantly narrow band gap. These results provide valuable insights into the design and development of new BODIPY dyes with tailored properties for various applications.