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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
Mon Mar 15 2021
Journal Name
Al-academy
Semiotics of Musical Sign in Iraqi Pantomime Show (Ahriman) as a Model: علي عدي صاحب-شيماء حسين طاهر
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The musical sign was associated with the first appearances of acting that are based on human gestures and expressive and silent movements, and they contributed in accentuating and clarifying these gestures and explain their meanings and indications, and they remained with them until these gestures turned into artistic theatrical shows so that the musical sign would have many functions and constitute the main pillars for this kind of show.
The musical sign is a language not much different than the human language in the semiotic analysis. There has been an increased interest in it and its use in the mime shows by the graduates who realized its necessity and significance in the pantomime show intellectually, artistically and aesthetical

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Publication Date
Sun Apr 01 2018
Journal Name
Journal Of Educational And Psychological Researches
The obstacles that encounter a program of rehabilitating released prisoners as perceived by prisoners themselves in tubas' province
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The study intends to explore the obstacles that encounter a program of rehabilitating released prisoners as perceived by prisoners themselves in tubas' province. To this end, the researcher used a questionnaire as an instrument which was applied on (150) prisoner had chosen randomly to collect the study data. The findings revealed no significant differences among obstacles the encounter program regarding to the following variables: age, detention period, and number of detention, additionally, the findings found that there is a variance of obstacles mean according to the prisoners themselves, rehabilitation program, and the facility of that program.

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Publication Date
Sun Apr 03 2022
Journal Name
Iraqi Journal Of Laser
On the use of Aluminium as a plasmonic material in polarization rotators based on a hybrid plasmonic waveguide
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: The Aluminium (Al) material emerged as a plasmonic material in the wavelength ranges from the ultraviolet to the visible bands in different on-chip plasmonic applications. In this paper, we demonstrate the effect of using Al on the electromagnetic (EM) field distribution of a compact hybrid plasmonic waveguide (HPW) acting as a polarization rotator. We compare the performance of Al with other familiar metals that are widely used as plasmonic materials, which are Silver (Ag) and Gold (Au). Furthermore, we study the effect of reducing the geometrical dimensions of the used materials on the EM field distributions inside the HPW and, consequently, on the efficiency of the polarization rotation. We perform the study based o

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Publication Date
Sun Feb 10 2019
Journal Name
Iraqi Journal Of Physics
A study of the effect of acid immersion on some physical properties of ( Epoxy – MgO) composites
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In this study a polymeric composite material was prepared by hand
lay-up technique from epoxy resin as a matrix and magnesium oxide
(MgO) as a reinforcement with different weight fraction (5,10,15,
and 20)% to resin. Then the prepared samples were immersed under
normal condition in H2So4(1 M) solution, for periods ranging up to
10 weeks. The result revealed that the diffusion coefficient
decreasing as the concentration of MgO increase. Also we studied
Hardness for the prepared samples before and after immersion. The
result revealed that the hardness values increase as the concentration
of MgO increase, while the hardness for the samples after immersion
in H2SO4 dec

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Publication Date
Mon Jul 01 2019
Journal Name
Journal Of Engineering
The Characters of the Form in the Vernacular Architecture A comparative study of the form's characters of facades of individual houses and commercial buildings in the City of Baghdad after 2003–Zayoona district as a case study
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The characters of facades' form of the Iraqi building after 2003 have been changed, it has been described by many names. The problem of the research is that what are the features of the characters of the form in the façades of the buildings in Baghdad city after 2003? Are the façade of the individual houses or the commercial buildings is the heaviest in the visual weight? The research aims to answer those questions by choosing the vernacular architecture as a measurement tool. It is the informal image of the architecture, which is built by people informally and spontaneously, without official control and legislation to be organized. This is smellier to what has happened in Baghdad, after 2003 according to previous stud

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Publication Date
Sun Dec 01 2019
Journal Name
Baghdad Science Journal
Extraction, Purification and Characterization of Peroxidase from Pseudomonas aeruginosa and Utility as Antioxidant and Anticancer
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        Peroxidase is a class of oxidation-reduction reaction enzyme that is useful for accelerating many oxidative reactions that protect cells from the harmful effects of free radicals. Peroxidase is found in many common sources like plants, animals and microbes and have extensive uses in numerous industries such as industrial, medical and food processing. In this study, P. aeruginosa was harvested to utilize and study its peroxidases. P. aeruginosa was isolated from a burn patient, and the isolate was verified as P. aeruginosa using staining techniques, biochemical assay, morphological, and a sensitivity test. The gram stain and biochemical test result show rod pink gram-ne

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Publication Date
Mon Jan 01 2024
Journal Name
Proceedings Of The 31th Minisymposium
Towards the Requirement-Driven Generation and Evaluation of Hyperledger Fabric Network Designs
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Publication Date
Sat May 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Evaluation Yield of Okra with Associated Traits Using Analysis Correlation and Path
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Abstract<p>The study was conducted at the fields of the Department of Horticulture and Landscape Gardening, College of Agriculture Engineering Sciences, University of Baghdad. During the spring 2017. All the recommended practices were followed during experimentation. The experimental material consisted four Genotype it is Batraa, Btera, Mosulle, and local selection. The experiment was applied in Randomized Complete Block Design (RCBD). The objectives of Study were to estimate the some genetic parameters and path coefficient for some traits Okra, The results of statistical analysis for these genotypes were highly significant differences for all traits except the traits number of leaves, the numbe</p> ... Show More
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Publication Date
Wed Aug 13 2025
Journal Name
Mechanics Of Time-dependent Materials
Performance evaluation of highly modified asphalt binders using elastomeric and plastomeric polymers
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Highly Modified Asphalt (HiMA) binders have garnered significant attention due to their superior resistance to rutting, fatigue cracking, and thermal distress under heavy traffic loads and extreme environmental conditions. While elastomeric polymers such as Styrene- Butadiene-Styrene (SBS) have been extensively used in HiMA applications, the potential of plastomeric polymers, including Polyethylene (PE) and Ethylene Vinyl Acetate (EVA), remains largely unexplored. This study aims to evaluate the performance of reference binder (RB) modified with plastomeric HiMA asphalt in comparison to SBS-modified binders and determine the optimal polymer dosage for achieving an optimal balance between rutting resistance and fatigue durability. The experi

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Publication Date
Tue Sep 30 2014
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Evaluation of Hydrocarbon Saturation Using Carbon Oxygen (CO) Ratio and Sigma Tool
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The main aim of this study is to evaluate the remaining oil in previously produced zones, locate the water productive zone and look for any bypassed oil behind casing in not previously perforated intervals. Initial water saturation was calculated from digitized open hole logs using a cut-off value of 10% for irreducible water saturation. The integrated analysis of the thermal capture cross section, Sigma and Carbon/oxygen ratio was conducted and summarized under well shut-in and flowing conditions. The logging pass zone run through sandstone Zubair formation at north Rumaila oil field. The zones where both the Sigma and the C/O analysis show high remaining oil saturation simila

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