Browsing by Author "Işgör,B.S."

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Indole Derivatives as Src Family Kinase and Glutathione S-Transferase Inhibitors: Evaluation of Their Selectivity and Drug Resistance Properties;
(2012) Işgör,B.S.; Kiliç Kurt,Z.; Işgör,Y.G.; Ölgen,S.; 01. Atılım University
The increased activity levels of Glutathione S-transferases (GST) have been correlated with human cancers and the anticancer drug resistance. Similarly, Src family kinases (SFKs), has been reported in many cancers including breast, colon, lung, and skin with relatively high catalytic activity. Therefore, the inhibition of both GSTs and Src may enhance the therapeutic efficacy of chemotherapeutics by increasing the selectivity and resistance of compounds. The recent efforts of our laboratory to design and synthesize novel c-Src inhibitors were accomplished with four indole-3-amine derivatives substituted at N1 and C5 (8c, 8f 8g, and 8h), with IC 50s values of 4.69, 74.79, 75.06, and 84.23 μM, respectively. In this present work, the inhibitory activities against SFKs (Lyn, Hck, Fyn), GSTs and selectivity studies of these compounds were performed. Among the compounds, 8c and 8g are found the best GST inhibitors with IC 50s values of 120.1, and 67.33 μM, respectively, and are reported as the Src inhibitors with dual action. The compounds 8f and 8h are also showed reasonable inhibitory levels of GSTs with IC 50s of 161.1, and 272.2 μM, However inhibition profiles of compounds are not found suitable for further developments.
Modeling Surface Water Quality and Nutrient Correlation With Sediment Oxygen Demand at Dam Water Reservoirs
(Technoscience Publications, 2022) Abdulqader,N.N.; Işgör,B.S.; Genç,A.N.; Güler,E.; Seymenoǧlu,V.C.; Department of Civil Engineering; Chemical Engineering; 15. Graduate School of Natural and Applied Sciences; 06. School Of Engineering; 01. Atılım University
The work presented here is a model approach based on WASP8 (Water analysis simulation program) a water quality model simulated to represent contaminants at the surface and bottom sediments of Kurtboǧazi dam reservoir in Ankara city. However, our water quality output variables: are temperature, nitrate, total phosphorus, total Kjeldahl nitrogen, dissolved oxygen, Chlorophyll a, and ammonia. To ensure the model represents the actual case at the reservoir, the results from the simulation model were calibrated using actual data from the Kurtboǧazi dam site, the calibration utilizes statistical techniques. The first method was the goodness-of-fit, R2 between model variables and field data, and the results were in the range of 0.86 to 1.0 indicating excellent linear association. The second technique was the RE, the values of which obtained were less than 1, elaborating acceptable results. The dam reservoir Kurtboǧazi had been affected by the negative impact arising from dissolved oxygen depletion in the hypolimnetic layer during stratification periods and that had been well documented. However, the processes of oxygen consumption at the sediment-water interface are still difficult to grasp conceptually and mainly linked to sediment oxygen depletion and the phenomena of sediment oxygen demand SOD. The novelty of this research work is the development of a quality model to predict the reactions of state variables that are occurring at the water body and how they interact with each other and their influence on the overall quality status of the Kurtboǧazi reservoir, and the crucial factors influencing the depletion of oxygen at the water column; secondly, the effect of anoxic condition on the benthic flux and the impact of anoxia condition on the ratio of nitrogen to phosphorus ratio at the reservoir. It was evident from the results of calibration that the model successfully simulated the correlation of the parameters influencing the anoxic condition, and benthic flux and ratio shift from nitrogen-limited during the summer to phosphorus-limited at the beginning of winter. © 2022 Technoscience Publications. All rights reserved.
Citation - Scopus: 6
Synthesis and Biological Study of Novel Indole-3 Derivatives as Src Kinase and Glutathione S-Transferase Inhibitors
(Bentham Science Publishers, 2013) Kurt,Z.K.; Aydin,D.; Işgör,Y.G.; Işgör,B.S.; Olgen,S.; 01. Atılım University
The aim of this study is to design and synthesize novel dual inhibitors of Src protein tyrosine kinase (PTK) and Glutathione S-transferases (GSTs), as a potential drug lead with therapeutic efficacy on cancer and immune disorders. The biological activity profiling of small molecule inhibitors via miniaturized biochemical techniques compatible with medium throughput screening and focused screening methodologies were performed. To determining the effects of small molecule inhibitors on Src kinase and Phase II detoxification enzyme GST isozymes in liver homogenates used to verify their roles in drug resistance mechanism for cancer chemotherapeutics. In this study, 14 indole-3-imine-2-on and N-benzyl indole-3-imine-2-on derivatives were synthesized for dual activities against Src and GST. The chemical structures and purities of compounds were verified by IR, 1H NMR, MASS spectroscopy, and elemental analysis. The compounds 2, 3 and 9 are found slightly active against both enzyme Src and GST. © 2013 Bentham Science Publishers.