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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 Feb 12 2022
Journal Name
Engineering, Technology & Applied Science Research
Prestressing Effects on Full Scale Deep Beams with Large Web Openings¨: An Experimental and Numerical Study
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Most studies on deep beams have been made with reinforced concrete deep beams, only a few studies investigate the response of prestressed deep beams, while, to the best of our knowledge, there is not a study that investigates the response of full scale (T-section) prestressed deep beams with large web openings. An experimental and numerical study was conducted in order to investigate the shear strength of ordinary reinforced and partially prestressed full scale (T-section) deep beams that contain large web openings in order to investigate the prestressing existence effects on the deep beam responses and to better understand the effects of prestressing locations and opening depth to beam depth ratio on the deep beam performance and b

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Publication Date
Fri Sep 30 2011
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Experimental Study on Carbon Steel Corrosion and its Inhibition Using Sodium Benzoate Under Different Operating Conditions
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Corrosion experiments were carried out to investigate the effect of several operating parameters on the corrosion rate and corrosion potential of carbon steel in turbulent flow conditions in the absence and presence of sodium benzoate inhibitor using electrochemical polarization technique. These parameters were rotational velocity (0 - 1.57 m/s), temperature (30oC – 50oC), and time. The effect of these parameters on the corrosion rate and inhibition efficiency were investigated and discussed. It was found that the corrosion rate represented by limiting current increases considerably with increasing velocity and temperature and that it decreased with time due to the formation of corrosion product layer. The corrosion potential shifted t

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Publication Date
Wed Jun 17 2026
Journal Name
Revista Iberoamericana De Psicología Del Ejercicio Y El Deporte, Issn 1886-8576, Vol. 17, Nº. 6, 2022, Págs. 405-407
Bullying behavior and its relationship to achievement motivation for young football players under (19) years old
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Autoría: Muwafaq Obayes Khudhair. Localización: Revista iberoamericana de psicología del ejercicio y el deporte. Nº. 6, 2022. Artículo de Revista en Dialnet.

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Publication Date
Sun Mar 20 2016
Journal Name
Al-academy
Technological development and its association with the formal change to devices Flatiron: يوجل عبد الحسين فارس
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Evolution in the modern era Which led to the rapid change in the forms of industrial products For many reasons, So put current research into question the view (What are the design requirements that define the formal change in the Iron clothes)? To reach the aim of In the design cornerstonesUnderlying the formal changethe Iron of the clothes, In the first section shed light on the development stages of systems design lists the historic stages of development and energy operator devices irons and mechanism of action and internal components, while in the second part, which was entitled (The role of technology and the factors influencing the change formality of Iron) touched on the three topics which technology modern industrial and receiver,

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Publication Date
Sat Jun 15 2019
Journal Name
Agriculture
Cover Crop Influence on Soil Enzymes and Selected Chemical Parameters for a Claypan Corn–Soybean Rotation
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Cover crops (CC) improve soil quality, including soil microbial enzymatic activities and soil chemical parameters. Scientific studies conducted in research centers have shown positive effects of CC on soil enzymatic activities; however, studies conducted in farmer fields are lacking in the literature. The objective of this study was to quantify CC effects on soil microbial enzymatic activities (β-glucosidase, β-glucosaminidase, fluorescein diacetate hydrolase, and dehydrogenase) under a corn (Zea mays L.)–soybean (Glycine max (L.) Merr.) rotation. The study was conducted in 2016 and 2018 in Chariton County, Missouri, where CC were first established in 2012. All tested soil enzyme levels were significantly different between 2016 and 2018

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Publication Date
Fri Oct 01 2010
Journal Name
2010 Ieee Symposium On Industrial Electronics And Applications (isiea)
Distributed t-way test suite data generation using exhaustive search method with map and reduce framework
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Publication Date
Thu Apr 15 2021
Journal Name
Biochem. Cell. Arch.
CYTOKINES PROFILE FOR INTESTINAL AND SPLEEN HOMOGENATE FOR IMMUNOSUPPRESSANT BALB/C MICE INFECTED WITH CRYPTOSPORIDIUM PARVUM
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Cryptosporidiosis is mainly cause a persistent diarrhea in immune compromised patients, BALB/c mice have been suppressed by dexamethasone, tissue Th1, Th2 and Th17 cytokines concentrations in the ileum were significantly diminished in both infected and immunosuppressed mice. Level of IFN-g, TNF-a, IL-12, IL-6, IL-17A was increased in level, IL-4 didn’t increases, in both ileal and spleen tissue. Levels of above cytokines were examined in spleen in order to follow the proliferation of CD4+ T-cell during C. parvum infection.

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Publication Date
Wed Nov 27 2024
Journal Name
International Journal Of Integrated Engineering
Noise Modeling and Removal from Electrocardiogram Signals: A Study Using Wavelet Transform with Graphical User Interface
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Publication Date
Sun May 10 2015
Journal Name
Al-academy
The industrial design aesthetic and its relationship with the recipient: باسم قاسم الغبان، صلاح نوري الجيلاوي
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The research problem lies in determining the beauty ranges between the receiver and the industrial product, The goal of the research, it is the definition of aesthetics in industrial design and its relation to the receiver, and the researcher outcome several conclusions of the, the most important was: 1. The role of accumulated experience, and their interaction with the vision of the artwork in achieving aesthetic perception and levels of artistic and aesthetic values and by the level of growth this taste of the recipient. 2. There are interactive and close relationship be the primary means for the integration of functional and aesthetic meaning the designer meant to get it to the receiver.

 

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Publication Date
Wed Jun 17 2026
Journal Name
Journal Mustansiriyah Of Sports Science
Self-Efficacy and its Relationship to Psychological Adjustment among Table Tennis Players with Disabilities Special Needs
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The introduction and importance of the research included that physical education and its various activities are important for the disabled. The exercise of physical activities by the disabled effectively contributes to raising their level of fitness and reducing diseases caused by lack of movement. Disabled people often suffer from psychological and social problems, and this feeling may be accompanied by a high level of anxiety, a lack of self-esteem and a loss of self-confidence. Psychological adaptation is one of the concepts of sports psychology interconnected with the psychological climate, as the process that the player seeks to meet his demands and needs. Adaptation includes the pursuit of emotional balance between the individual play

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