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Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

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Publication Date
Sat Oct 30 2021
Journal Name
Iraqi Journal Of Science
Recursive Prediction for Lossless Image Compression
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     This paper introduced an algorithm for lossless image compression to compress natural and medical images. It is based on utilizing various casual fixed predictors of one or two dimension to get rid of the correlation or spatial redundancy embedded between image pixel values then a recursive polynomial model of a linear base is used.

The experimental results of the proposed compression method are promising in terms of preserving the details and the quality of the reconstructed images as well improving the compression ratio as compared with the extracted results of a traditional linear predicting coding system.

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Publication Date
Fri Jan 01 2021
Journal Name
Advances In Intelligent Systems And Computing
Optimal Prediction Using Artificial Intelligence Application
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Publication Date
Wed Feb 01 2023
Journal Name
Periodicals Of Engineering And Natural Sciences (pen)
Bitcoin Prediction with a hybrid model
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In recent years, Bitcoin has become the most widely used blockchain platform in business and finance. The goal of this work is to find a viable prediction model that incorporates and perhaps improves on a combination of available models. Among the techniques utilized in this paper are exponential smoothing, ARIMA, artificial neural networks (ANNs) models, and prediction combination models. The study's most obvious discovery is that artificial intelligence models improve the results of compound prediction models. The second key discovery was that a strong combination forecasting model that responds to the multiple fluctuations that occur in the bitcoin time series and Error improvement should be used. Based on the results, the prediction acc

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Publication Date
Tue Feb 28 2023
Journal Name
Periodicals Of Engineering And Natural Sciences (pen)
Bitcoin Prediction with a hybrid model
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. In recent years, Bitcoin has become the most widely used blockchain platform in business and finance. The goal of this work is to find a viable prediction model that incorporates and perhaps improves on a combination of available models. Among the techniques utilized in this paper are exponential smoothing, ARIMA, artificial neural networks (ANNs) models, and prediction combination models. The study's most obvious discovery is that artificial intelligence models improve the results of compound prediction models. The second key discovery was that a strong combination forecasting model that responds to the multiple fluctuations that occur in the bitcoin time series and Error improvement should be used. Based on the results, the prediction a

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Publication Date
Thu Sep 01 2022
Journal Name
Computers And Electrical Engineering
Automatic illness prediction system through speech
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Publication Date
Wed Feb 01 2023
Journal Name
Baghdad Science Journal
Evaluation of Beta-2 Integrin and Platelets Roles in Sickle Cell Disease Pathogenicity in Basrah Governorate Patients
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Sickle cell disease (SCD) comprises an inherited blood disorder that is life long and affects many people globally. In spite of the development in treatment, SCA is a considerable cause of mortality and morbidity. The present study tries to assess the role of leukocytes represented by β integrin(CD18) and platelets and their productivity in the pathogenicity of disease during  the steady state and crisis in comparison with the healthy as-control group, SCD patients (15) enrolled during crisis and steady state (follow up) showed a significant increase in leukocytes and platelets cells productivity during crisis when compared to the steady state and in the steady state when compared to the healthy control group . In this study, SCD patho

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Publication Date
Thu Mar 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
The Role Of Information Technology In Enhancing Performance Evaluation And Responsibility Accounting (Empirical Study In Jordan Hotels )
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   This paper suggesting a new modern method to evaluate the performance of hotel industry at Jordan instead of the classical method used by the industry and that is Bench Marking , this method can be done by comparing the performance of hotel industry at two serial years which helps in calculating a standard performance .

  The industry can use this standard to identify the variance, which make the evaluation of performance easier and support the efforts to develop the hotel industry at all levels and enable to give high quality services to customers.

    The study believed that this situation would not be achieved unless the hotel industry will app

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Publication Date
Sun Apr 30 2023
Journal Name
Iraqi Journal Of Science
Evaluation of Three Important Electrode Arrays in Defining the Vertical and Horizontal Structures in 2D Imaging Surveys
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Three important electrode arrays in 2D imaging surveys were tested in this study through synthetic model to determine which array is the most successful in defining the vertical and horizontal geological structures. These arrays are Wenner-Schlumberger, Wenner and Dipole - dipole. The numerical modeling was created through vertical fracture zone and three separate cavities surrounded by horizontal layers. The results showed that the Wenner-Schlumberger is the most suitable electrode array when both vertical and horizontal structures are present in the subsurface. It is the best in imaging the vertical and horizontal contacts and represented these structures more accurately than the Wenner and Dipole-dipole arrays.

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Publication Date
Fri Jan 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Evaluation of Heavy Metals Concentration in Street, Storm and Suspended Dust in Al-Zafaraniya Area, Baghdad- Iraq
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The current study was applied in Al-Zafaraniya area southeast of the capital Baghdad from October 2021 to April 2022. This is to evaluate some heavy elements (Cd, Co, Cu, Fe, Pb, and Mn) in the street, storm, and suspended dust. Four sampling sites were selected, and codes A, B, C, and D were given to represent the industrial activity sites, service workshops, business activity, and residential areas.

        The results showed that the concentration rates of elements (Cd, Co, Cu, Fe, Pb, Mn) in street dust samples were (1.15, 6.6, 60.15, 26770, 44.4, 6, 489.8). In storm dust (2, 10, 49.3, 54760, 24.3, 827.2) ppm, respectively, the results of suspended dust revealed that the general rates of element concentrations were (0.7

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Publication Date
Sun Dec 30 2018
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Prediction of penetration Rate and cost with Artificial Neural Network for Alhafaya Oil Field
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Prediction of penetration rate (ROP) is important process in optimization of drilling due to its crucial role in lowering drilling operation costs. This process has complex nature due to too many interrelated factors that affected the rate of penetration, which make difficult predicting process. This paper shows a new technique of rate of penetration prediction by using artificial neural network technique. A three layers model composed of two hidden layers and output layer has built by using drilling parameters data extracted from mud logging and wire line log for Alhalfaya oil field. These drilling parameters includes mechanical (WOB, RPM), hydraulic (HIS), and travel transit time (DT). Five data set represented five formations gathered

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