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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
Fri Oct 01 2021
Journal Name
Journal Of Engineering
Some Geotechnical Properties of Plastic Soil Enhanced with Cement Dust
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Plastic soil exhibits unfavorited geotechnical properties (when saturation), which causes negative defects to engineering structures. Different attempts (included various materials) were conducted to proffer solutions to such defects by experimenting in practical ways. On one hand, these attempts aimed to improve the engineering characteristics of plastic soil, and on the other hand, to use problematic waste materials as a stabilizer, like cement kiln dust, and to reduce environmental hazards. This paper explored the shrinkage, plasticity, and strength behavior of plastic soil enhanced with cement dust. The cement dust contents were 0%, 5%, 10%, 15% and 20% by dry weight of soil. An experimental series of shrinkage and p

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Publication Date
Sat Mar 22 2025
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Snare-Assisted Retrieval of an Embolized Broken Double Lumen from the Heart of a Female Patient Diagnosed with End Stage Kidney Disease: A Case Report
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Foreign body embolization is a rare but serious iatrogenic complication that might necessitate transcatheter or even surgical retrieval. A broken double-lumen catheter was snared using a goose neck snare kit. The procedure was successful, and the patient experienced no further complications.

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Publication Date
Mon Jul 04 2016
Journal Name
University Of Plymouth
‘History Engraved on his Shoulder’: A Comparative Study of the Influence of British First World War Poetry on Post 1980 Iraqi War Poetry "embargoed indefinitely"
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Abstract This study aims to compare British war poetry of the First World War with Iraqi poetry from the mid-20th century with special reference to Iraqi war poetry of the 1980’s Iraq-Iran War and the period that followed it. It will also investigate the influence of the designated British war poetry on the chosen body of Iraqi poetry. Through the comparison of sample poems the study presents, firstly, the direct influence of the British poetry of the Great War and its translation which formed the seeds of a more radical movement in Iraqi poetry during the 1980’s Iran/Iraq War and the period that followed it. The study also presents a comparison of the works of British and Iraqi civilian poets during and after the war time and their con

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Publication Date
Sun Jul 26 2026
Journal Name
Journal Of Economics And Administrative Sciences
The effect of creating knowledge according to the model (Nonaka & Takeuchi, 1995) on organizational ambidexterity: A study on a sample of Iraqi private banks
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Purpose - This study relies on the descriptive and analytical approach through collecting and analyzing the necessary data, as this approach focuses on polling the opinions of the research sample and its directions, and aims to develop a model that studies the relationship between knowledge creation and organizational ambidexterity in Iraqi private banks and verifying its validity experimentally. Design / Methodology / Introduction - A survey was conducted through a questionnaire form to collect data from a sample of (113) managers in private commercial banks. In addition, this study used the AMOS program and the ready-to-use statistical program package (SPSS V.25) to test the proposed hypotheses of the theoretical model experimentally. Res

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Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
Multiple Intelligence Test Item Selection-Based on Howard Gardner's MI Model Using a Generalized Partial Estimation Model: Ministry of Education \ Karkh First Directorate of Education
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The aim of the research is to examine the multiple intelligence test item selection based on Howard Gardner's MI model using the Generalized Partial Estimation Form, generalized intelligence. The researcher adopted the scale of multiple intelligences by Kardner, it consists of (102) items with eight sub-scales. The sample consisted of (550) students from Baghdad universities, Technology University, al-Mustansiriyah university, and Iraqi University for the academic year (2019/2020). It was verified assumptions theory response to a single (one-dimensional, local autonomy, the curve of individual characteristics, speed factor and application), and analysis of the data according to specimen partial appreciation of the generalized, and limits

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Publication Date
Tue Jan 31 2017
Journal Name
Journal Of Engineering
A Study on the Removal of Direct Blue 71 Dye From Textile Wastewater Produced From State Company of Cotton Industries by Electrocoagulation Using Aluminum Electrodes
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The removal of direct blue 71 dye from a prepared wastewater was studied employing batch electrocoagulation (EC) cell. The electrodes of aluminum were used. The influence of process variables which include initial pH (2.0-12.0), wastewater conductivity (0.8 -12.57) mS/cm , initial dye concentration (30 -210) mg/L, electrolysis time  (3-12) min, current density (10-50) mA/cm2   were studied in order to maximize the color removal from wastewater. Experimental results showed that the color removal yield increases with increasing pH until pH 6.0 after that it decreased with increasing pH. The color removal increased with increasing current density, wastewater conductivity, electrolysis time, and decreased with increasing the concen

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Publication Date
Sun May 01 2022
Journal Name
Journal Of Ecological Engineering
Ability of Response Surface Methodology to Optimize Photocatalytic Degradation of Amoxicillin from Aqueous Solutions Using Immobilized TiO<sub>2</sub>/Sand
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Publication Date
Thu Jun 29 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Emulsion Liquid Membrane for Pesticides Removal from Aqueous Solution: Emulsion Stability, Extraction Efficiency and Mass Transfer Studies
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The current study investigated the stability and the extraction efficiency of emulsion liquid membrane (ELM) for Abamectin pesticide removal from aqueous solution. The stability was investigated in terms of droplet emulsion size distribution and emulsion breakage percent. The proposed ELM included a mixture of corn oil and kerosene (1:1) as a diluent, Span 80 (sorbitan monooleate) as a surfactant and hydrochloric acid (HCl) as a stripping agent without utilizing a carrier agent. Parameters such as homogenizer speed, surfactant concentration, emulsification time and internal to organic volume ratio (I/O) were evaluated. Results show that the lower droplet size of 0.9 µm and higher stable emulsion in terms of breakage percent of 1.12 % were

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Publication Date
Wed Sep 01 2021
Journal Name
Baghdad Science Journal
On Comparison Study between Double Sumudu and Elzaki Linear Transforms Method for Solving Fractional Partial Differential Equations
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        In this paper, double Sumudu and double Elzaki transforms methods are used to compute the numerical solutions for some types of fractional order partial differential equations with constant coefficients and explaining the efficiently of the method by illustrating some numerical examples that are computed by using  Mathcad 15.and graphic in Matlab R2015a.

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Publication Date
Thu Oct 18 2018
Journal Name
European Journal Of Organic Chemistry
PdII-Mediated Oxidative Amination for Access to a 9-Azabicyclo[4.2.1]nonane Compound Library and Anatoxin-a
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