Person: BİNGÖL ÖZAKPINAR, ÖZLEM
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BİNGÖL ÖZAKPINAR
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ÖZLEM
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Publication Metadata only Molecular modeling and assessment of cytotoxic and apoptotic potentials of imatinib analogues featuring (thio)urea motifs in human leukemia and lymphoma cells(MARMARA UNIV, 2020) TÜRE, ASLI; Bingol Ozakpinar, Ozlem; Ture, Asli; Kucukguzel, IlkayImatinib is a well-known anticancer drug. In this study, cytotoxic properties of thirty-two imatinib analogues featuring (thio)urea motifs have been evaluated against chronic myeloid leukemia (K562), Burkitt lymphoma (Raji) and mouse embryonic fibroblast (NIH 3T3) cells. IC50 values of selected eleven compounds were calculated against K562 and NIH 3T3 cells. Apoptotic properties of the most active three compounds were evaluated on K652 cells subsequently. Favorably, compounds 19, 31 and 32 induced early apoptotic changes on K562 cells. Loss of membrane potential as well as caspase-3 and caspase-9 activation was determined in the present study. Levels of anti-apoptotic proteins, Bcl-XL and Bcl-2 decreased after the implementation of compounds 19, 31 and 32 at 10 mu M and 50 mu M concentrations. To reveal further molecular insight into the anticancer activity of the compounds, compounds 19, 31 and 32 were docked into ABL kinase protein as imatinib shows anticancer activity by inhibiting this enzyme. Modeling studies demonstrated significant molecular interactions between compounds 19, 31 and 32 and ABL protein. Compounds 19, 31 and 32 showed excellent superposition with imatinib in the binding site of ABL. These findings suggest that compounds 19, 31 and 32 have potential to show anticancer activity against chronic myeloid leukemia.Publication Metadata only Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2016) ÖZSAVCI, DERYA; Kulabas, Necla; Tatar, Esra; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Pannecouque, Christophe; De Clercq, Erik; Kucukguzel, IlkayIn this study, a series of thiosemicarbazide derivatives 12-14, 1,2,4-triazol-3-thione derivatives 15-17 and compounds bearing 2-(4H-1,2,4-triazole-3-ylthio)acetamide structure 18-32 have been synthesized starting from phenolic compounds such as 2-naphthol, paracetamol and thymol. Structures and purity of the target compounds were confirmed by the use of their chromatographic and spectral data besides microanalysis. All of the synthesized new compounds 12-32 were evaluated for their anti-HIV activity. Among these compounds, three representatives 18, 19 and 25 were selected and evaluated by the National Cancer Institute (NCI) against the full panel of 60 human cancer cell lines derived from nine different cancer types. Antiproliferative effects of the selected compounds were demonstrated in human tumor cell lines K-562, A549 and PC-3. These compounds inhibited cell growth assessed by MTT assay. Compound 18,19 and 25 exhibited anti-cancer activity with IC50 values of 5.96 mu M (PC-3 cells), 7.90 mu M (A549/ATCC cells) and 7.71 mu M (K-562 cells), respectively. After the cell viability assay, caspase activation and Bcl-2 activity of the selected compounds were measured and the loss of mitochondrial membrane potential (MMP) was detected. Compounds 18, 19 and 25 showed a significant increase in caspase-3 activity in a dose-dependent manner. This was not observed for caspase-8 activity with compound 18 and 25, while compound 19 was significantly elevated only at the dose of 50 mu M. In addition, all three compounds significantly decreased the mitochondrial membrane potential and expression of Bcl-2. (C) 2016 Elsevier Masson SAS. All rights reserved.Publication Metadata only Synthesis and Biological Activity of N-(arylsulfonyl) Valine Hydrazones and Assistance of NMR Spectroscopy for Definitive 3D Structure(BENTHAM SCIENCE PUBL LTD, 2019) TATAR, ESRA; Senkardes, Sevil; Tatar, Esra; Nepravishta, Ridvan; Cela, Dorisa; Paci, Maurizio; Ozakpinar, Ozlem Bingol; Sekerler, Turgut; De Clercq, Erik; Pannecouque, Christophe; Kucukguzel, S. Guniz; Kucukguzel, IlkayBackground: Hydrazide-hydrazones constitute an important class of compounds for new drug development. In this study, a series of 39 new acylhydrazones (3-41), derived from (2S)-3-methyl-2-[[( 4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide were synthesized with further aim to achieve biologically active acylhydrazones carrying an amino acid side chain. Methods: Compounds 3-41 were synthesized by microwave-assisted method. All synthesized compounds have been tested for their anti-HIV activity compound 21 was subjected to a new set of 2D-NMR analysis for the characterization of the isomers in solution and determination of its 3D structure. Results: The IC50 values for compounds 2-40 were found between >125-10.90 mu g/ml against HIV-1( IIIB) and HIV-2(ROD) strains in MT-4 cells. Compounds 3, 6, 10, 12, 23, 24, 27, 32, and 37 with CC50 values between 10.90-14.50 mu g/ml were selected to evaluate for their antileukemia activity. IC50 values for these mentioned compounds were found as >100 mu M on human chronic myelogenous leukemia, K562 cell line. Conclusion: Some compounds with IC50 values between 10.90-14.50 mu g/ml will be of benefit in the development of novel leads.Publication Metadata only Synthesis, molecular modeling, anti-cancer and COX-1/2 inhibitory activities of novel thiazolidinones containing benzothiazole core(2024-01-01) KULABAŞ, NECLA; BİNGÖL ÖZAKPINAR, ÖZLEM; KÜÇÜKGÜZEL, İLKAY; KULABAŞ N., Guven C. T., Duracik M., BİNGÖL ÖZAKPINAR Ö., Kucukguzel I.In this study, new 1,3-thiazolidin-4-one derivatives containing arylmethylene groups in the 5-position were obtained from 6-(trifluoromethoxy)-1,3-benzo-thiazol-2-amine (riluzole). Synthesized compounds were characterized by spectral data and elemental analysis. In vitro, cytotoxic activities of the synthesized molecules were evaluated against the human lung cancer (A549) and human prostate cancer (PC-3) cell lines. Compounds were also tested on mouse embryonic fibroblast cells (NIH/3T3) to determine selectivity. Ten target compounds 3-12 were also screened for their COX-1 and COX-2 inhibitory activities. Of these compounds, 4 showed the highest COX-2 inhibition at 10 μM. Molecular docking calculations were performed to understand the binding interactions of compounds with COX-1 and COX-2 proteins. In silico studies of the tested compounds represented important binding modes that may be responsible for their anti-cancer activity via selective inhibition of the COX-2 enzyme. ADMET predictions were conducted to assess the drug-like properties of the novel compounds.