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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
Sun Jun 07 2015
Journal Name
Baghdad Science Journal
Serum Vascular Endothelial Growth Factor VEGF and Interlukin-8 As a Novel Biomarkers For Early Detection of Ovarian Tumors
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Epithelial ovarian cancer is the leading cause of cancer deaths from gynecological malignancies. Angiogenesis is considered essential for tumor growth and the development of metastases. VEGF and IL?8 are potent angiostimulatory molecules and their expression has been demonstrated in many solid tumors, including ovarian cancer.VEGF and IL-8 concentrations were measured by ELISA test (HumanVEGF,IL-8). Bioassay ELISA/ US Biological / USA).The median VEGF and IL-8 levels were significantly higher in the sera of ovarian cancer patients than in those with benign tumors and in healthy controls.Pretreatment VEGF and IL-8 serum levels might be regarded as an additional tool in the differentiation of ovarian tumors.

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Publication Date
Mon Sep 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Permeability Prediction in Carbonate Reservoir Rock Using FZI
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Knowledge of permeability, which is the ability of rocks to transmit the fluid, is important for understanding the flow mechanisms in oil and gas reservoirs.
Permeability is best measured in the laboratory on cored rock taken from the reservoir. Coring is expensive and time-consuming in comparison to the electronic survey techniques most commonly used to gain information about permeability.
Yamama formation was chosen, to predict the permeability by using FZI method. Yamama Formation is the main lower cretaceous carbonate reservoir in southern of Iraq. This formation is made up mainly of limestone. Yamama formation was deposited on a gradually rising basin floor. The digenesis of Yamama sediments is very important due to its direct

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Publication Date
Wed Jan 06 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances
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Synthesis, Characterization And Biological Evaluation of Schiff Base And Ligand Metal Complexes of Some Drug Substances

Publication Date
Mon Jun 01 2009
Journal Name
Journal Of Economics And Administrative Sciences
Suggested method for modifying the site parameter
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     Estimating multivariate location and scatter with both affine equivariance and positive break down has always been difficult. Awell-known estimator which satisfies both properties is the Minimum volume Ellipsoid Estimator (MVE) Computing the exact (MVE) is often not feasible, so one usually resorts to an approximate Algorithm. In the regression setup, algorithm for positive-break down estimators like Least Median of squares typically recomputed the intercept at each step, to improve the result. This approach is called intercept adjustment. In this paper we show that a similar technique, called location adjustment, Can be applied to the (MVE). For this purpose we use the Minimum Volume Ball (MVB). In order

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Publication Date
Fri May 01 2020
Journal Name
Journal Of Engineering
Semi-Analytical Prediction of Flank Tool Wear in Orthogonal Cutting of Aluminum
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This study aims to model the flank wear prediction equation in metal cutting, depending on the workpiece material properties and almost cutting conditions. A new method of energy transferred solution between the cutting tool and workpiece was introduced through the flow stress of chip formation by using the Johnson-Cook model. To investigate this model, an orthogonal cutting test coupled with finite element analysis was carried out to solve this model and finding a wear coefficient of cutting 6061-T6 aluminum and the given carbide tool.

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Publication Date
Sun May 05 2024
Journal Name
Technium Business And Management
Measuring Blue Ocean Leadership activities in public organizations: field research in the Ministry of Communications
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This study aims to identify the level of application of blue ocean leadership activities in public organizations and to build a conceptual and cognitive framework around this concept. The study adopted a descriptive-analytical approach, and the research sample consisted of (95) individuals from the senior management working at the center of the Iraqi Ministry of Communications (director general, department manager, section head). The data analysis technique used is structural equation modeling (SEM) and the Statistical Package for the Social Sciences (SPSS). The results indicate that the senior management in the Ministry of Communications is working to adopt the blue ocean leadership style through its activities, but not to the leve

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Publication Date
Mon Mar 30 2009
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Prediction of bubble size in Bubble columns using Artificial Neural Network
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In the literature, several correlations have been proposed for bubble size prediction in bubble columns. However these correlations fail to predict bubble diameter over a wide range of conditions. Based on a data bank of around 230 measurements collected from the open literature, a correlation for bubble sizes in the homogenous region in bubble columns was derived using Artificial Neural Network (ANN) modeling. The bubble diameter was found to be a function of six parameters: gas velocity, column diameter, diameter of orifice, liquid density, liquid viscosity and liquid surface tension. Statistical analysis showed that the proposed correlation has an Average Absolute Relative Error (AARE) of 7.3 % and correlation coefficient of 92.2%. A

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Publication Date
Fri Oct 17 2025
Journal Name
Journal Of Pharmaceutical Health Services Research
Cost-effectiveness of on-demand rFVIIa vs prophylactic emicizumab in hemophilia a with inhibitors: clinical, QoL, and ICER-based field insights
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Abstract<sec> <title>Objective

To evaluate the cost-effectiveness of emicizumab compared to recombinant activated factor VII (rFVIIa) in Iraqi patients with hemophilia A and inhibitors.

Method

A retrospective cost-effectiveness analysis was conducted on 46 male patients with hemophilia A and inhibitors treated at a public children’s hospital in Baghdad. Data collection was conducted between November 2024 and March 2025. Clinical and economic data were retrospectively collected for a 12-m

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Publication Date
Mon May 01 2017
Journal Name
Journal Of Stored Products Research
Detection and prediction of Sitophilus oryzae infestations in triticale via visible and near-infrared spectral signatures
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Triticale is a hybrid of wheat and rye grown for use as animal feed. In Florida, due to its soft coat, triticale is highly vulnerable to Sitophilus oryzae L. (rice weevil) and there is interest in development of methods to detect early-instar larvae so that infestations can be targeted before they become economically damaging. The objective of this study was to develop prediction models of the infestation degree for triticale seed infested with rice weevils of different growth stages. Spectral signatures were tested as a method to detect rice weevils in triticale seed. Groups of seeds at 11 different levels (degrees) of infestation, 0–62%, were obtained by combining different ratios of infested and uninfested seeds. A spectrophotometer wa

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Publication Date
Mon Jan 01 2024
Journal Name
Kafkas Universitesi Veteriner Fakultesi Dergisi
Assessment of In-vitro Cytotoxicity and In-ovo Virucidal Antiviral Efficacy of Various Plant Extracts and Bioactive Molecules
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