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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
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Estradiol and Prolactin Serum Levels "In Premenopausal; and Postmenopausal" Women with ((Breast Cancer)) In Baghdad City
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Objective:To Evaluate of Estradiol and Prolactin hormones levels for Breast Cancer women in
Baghdad City.
Methodology: The current study was conducted on 60 breast cancer women and 40 apparently
healthy subjects to evaluate the levels of estradiol and prolactin "hormones in the serum" of
({premenopausal & postmenopausal}) breast cancer and healthy controle women. Estradiol and
prolactin hormones estimated for all cases by using the IMMULITE 2000 instrument that performs
chemiluminescent immunoassays results are calculated for each sample.Data were analysed using
SPSS-18.data of two groups was comparison by the student's t-test.
Results: The results showed a non significant""(P>0.05) elevation in the –mean

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Publication Date
Mon Apr 01 2019
Journal Name
Plant Archive
EFFECT OF SOME GROWTH REGULATORS ON THE MULTIPLICATION AND STIMULATING THE PRODUCTION OF THE VOLATILE OIL OF ROSEMARY OFFICINALIS IN VITRO
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The experiment was conducted at the plant tissue culture laboratory of the Department of Horticulture and Garden Engineering College of Agricultural Engineering Sciences, University of Baghdad, in order to study the effect of some growth regulators on propagation an stimulation production of volatile oil compounds of rosemary plant Rosmarinus officinlis using two vegetative parts (apical and lateral buds). Factorial experiment was implemented in completely randomized design with twenty replications. The results indicated that culturing the apical meristem on the medium Murashige and Skoog (MS) media with 0.5 mg.l-1 (BA) with 0.1 mg.l-1 of NAA gave the highest response rate of 100%. As for the doubling stage, the levels of BAA and IAA (Indol

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Publication Date
Mon Aug 01 2016
Journal Name
Journal Of Engineering
Performance Evaluation of the Investment Projects during the Implementation Phase (Najaf province as a case study)
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The construction project is a very complicated work by its nature and requires specialized knowledge to lead it to success. The construction project is complicated socially, technically and economically in its planning, management and implementation aspects due to the fact that it has many variables and multiple stakeholders in addition to being affected by the surrounding environment. Successful projects depend on three fundamental points which are cost-time, performance and specifications. The project stakeholder's objective to achieve best specifications and the cost-time frame stipulated in the contract.

The question is, was the optimum implementation accomplished? The provision for the success of the project

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Publication Date
Mon Sep 05 2016
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EVALUATION OF CHEMICAL AND MICROBIAL QUALITY FOR SOME BOTTLED WATER THAT AVAIABLE IN LOCAL MARKETS: EVALUATION OF CHEMICAL AND MICROBIAL QUALITY FOR SOME BOTTLED WATER THAT AVAIABLE IN LOCAL MARKETS
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This study was conducted to evaluate the bottled water quality for the six-producing companies in Baghdad city, where selected six brands which are the most marketed in the Iraqi market, especially in Baghdad, where taking the proper amount of bottled water in September 2015 and included the studied characteristics (EC , pH ,TDS, Turbidity, Ca+2, Mg+2, Cl-, No3-, So4-2, HCO3-, Na+ and K+) in addition to the total population of bacteria aerobic and coliform, and compare the results with the standard specifications of the Iraqi and the World Health Organization (WHO), as well as to compare the results of sampling specifications mentioned on the packaging by the producing companies. The results showed the presence of high significant differ

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Publication Date
Tue May 01 2018
Journal Name
Journal Of Engineering
Prediction of the Effect of Using Stone Column in Clayey Soil on the Behavior of Circular Footing by ANN Model
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Shallow foundations are usually used for structures with light to moderate loads where the soil underneath can carry them. In some cases, soil strength and/or other properties are not adequate and require improvement using one of the ground improvement techniques. Stone column is one of the common improvement techniques in which a column of stone is installed vertically in clayey soils. Stone columns are usually used to increase soil strength and to accelerate soil consolidation by acting as vertical drains. Many researches have been done to estimate the behavior of the improved soil. However, none of them considered the effect of stone column geometry on the behavior of the circular footing. In this research, finite ele

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Publication Date
Sun Jun 30 2013
Journal Name
Al-khwarizmi Engineering Journal
Efficiency Prediction and Performance Characterization of Photovoltaic Solar Panel at Baghdad Climate Conditions
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The performance of a solar cell under sun radiation is necessary to describe the electrical parameters of the cell. The Prova 200 solar panel analyzer is used for the professional testing of four solar cells at Baghdad climate conditions. Voltage -current characteristics of different area solar cells operated under solar irradiation for testing their quality and determining the optimal operational parameters for maximum electrical output were obtained. A correlation is developed between solar cell efficiency h and the corresponding solar cell parameters; solar irradiance G, maximum power Pmax, and production date P. The average absolute error of the proposed correlation is 5.5% for 40 data points. The results also show th

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Publication Date
Wed Sep 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
A Viscoplastic Modeling for Permanent Deformation Prediction of Rubberized and Conventional Mix Asphalt
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Publication Date
Fri Dec 30 2022
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Artificial Intelligent Models for Detection and Prediction of Lost Circulation Events: A Review
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Lost circulation or losses in drilling fluid is one of the most important problems in the oil and gas industry, and it appeared at the beginning of this industry, which caused many problems during the drilling process, which may lead to closing the well and stopping the drilling process. The drilling muds are relatively expensive, especially the muds that contain oil-based mud or that contain special additives, so it is not economically beneficial to waste and lose these muds. The treatment of drilling fluid losses is also somewhat expensive as a result of the wasted time that it caused, as well as the high cost of materials used in the treatment such as heavy materials, cement, and others. The best way to deal with drilling fluid losses

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Publication Date
Fri Jun 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Correlation for fitting multicomponent vapor-liquid equilibria data and prediction of azeotropic behavior
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Correlation equations for expressing the boiling temperature as direct function of liquid composition have been tested successfully and applied for predicting azeotropic behavior of multicomponent mixtures and the kind of azeotrope (minimum, maximum and saddle type) using modified correlation of Gibbs-Konovalov theorem. Also, the binary and ternary azeotropic point have been detected experimentally using graphical determination on the basis of experimental binary and ternary vapor-liquid equilibrium data.

            In this study, isobaric vapor-liquid equilibrium for two ternary systems: “1-Propanol – Hexane – Benzene” and its binaries “1-Propanol –

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Publication Date
Fri Dec 01 2023
Journal Name
Advances In Science And Technology Research Journal
Experimental Investigation and Fuzzy Based Prediction of Titanium Alloy Performance During Drilling Process
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