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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 Jul 13 2023
Journal Name
International Journal Of Research In Social Sciences & Humanities
Subject Review: Blogs as Learning Tools in EFL Classrooms
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Blogs have emerged as a powerful technology tool for English as a Foreign Language (EFL) classrooms. This literature review aims to provide an overview of the use of blogs as learning tools in EFL classrooms. The study examines the benefits and challenges of using blogs for language learning and the different types of blogs that can be used for language learning. It provides suggestions for teachers interested in using blogs as learning tools in their EFL classrooms. The findings suggest that blogs are a valuable and effective tool for language learning, particularly in promoting collaboration, communication, and motivation.

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Publication Date
Mon Mar 01 2010
Journal Name
Al-khwarizmi Engineering Journal
Synthetic Sacks as Reinforced Fibers in the Thermosetting Composites
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This study was carried out to investigate the preparation of thermosetting polymeric blend consisting of three adhesive types, namely: epoxy, polyvinyl formal (PVF) and unsaturated polyester. Both of epoxy and PVF were used as a matrix-binder at fixed weight. Whilst unsaturated polyester was used at different weights and added to the matrix so as to produce prepared epoxy-PVF-unsaturated polyester blend. Several experiments were performed at different operating conditions, mixing speed and time at room temperature to identify the most favorable operating conditions. The optimum mixing speed and mixing time for the prepared blend were 500rpm and 5 minutes respectively.

      Solid wastes-synthetic sack fib

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Publication Date
Wed Jan 01 2014
Journal Name
Journal Of The College Of Languages (jcl)
Tennessee Williams: Memories as symbols in The Glass Menagerie
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The Glass Manegerie is a metaphor, which is one of the greatest plays  of great writer Williams. The play talks about  the poor people in society and how try to escape this group of people from the real world to get rid of the hardness of this tuff reality and live in a fantasy world that is much like the glass where the world is very weak this world is acting by Laura, she is  owner of these animals breakable glass where it's weak and unable to defend itself as well as the mother Amanda  is a very selfish never think about her children but only herself.

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Publication Date
Sat Feb 01 2025
Journal Name
Iop Conference Series: Earth And Environmental Science
Chitosan as an Aflatoxin Inhibitor in Local Fish Feed
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Abstract<p>The current research attempts to find a feed additive that enhances fish growth and eliminate toxins generated from fungi and mold, which are found in improperly manufactured and stored feed, while ensuring the safety of these fish meat for the consumer. Therefore, the organic properties of chitosan powder were examined in order to determine its impact on maturation of young <italic>Cyprinus carpio</italic>. Chitosan was tested in three samples of feedings at three concentrations: CH1 7gm/1kg fish feed, CH2 10gm/1kg, and CH3 15gm/1kg carp fish feed. The results showed that the third parameter, 15gm CH3 chitosan/kg of feed, was superior to the other parameters, having a highl</p> ... Show More
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Publication Date
Wed Sep 01 2021
Journal Name
Journal Of Engineering
Spike neural network as a controller in SDN network
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The paper proposes a methodology for predicting packet flow at the data plane in smart SDN based on the intelligent controller of spike neural networks(SNN). This methodology is applied to predict the subsequent step of the packet flow, consequently reducing the overcrowding that might happen. The centralized controller acts as a reactive controller for managing the clustering head process in the Software Defined Network data layer in the proposed model. The simulation results show the capability of Spike Neural Network controller in SDN control layer to improve the (QoS) in the whole network in terms of minimizing the packet loss ratio and increased the buffer utilization ratio.

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Publication Date
Tue Nov 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Adoption of Membership Level for Critical Activities In Knowledge Chain Model Building An Investigation Analytical Study Depending on Fuzzy Logic Architecture for Organizations Pushed by Knowledge
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Abstract

   The aim of this research is to concentrate on the of knowledge management activities, initial activities: (Acquisition, Selection, Generation, Assimilation, Emission) knowledge, and support activities: (Measurement, Control, Coordination, Leadership) that is manipulate and controlling in achieving knowledge management cases in organization, that’s is leads to  knowledge chain model, then determining the level of membership for these activities to knowledge chain model in a sample of Iraqi organization pushed by knowledge (Universities). The research depends on check list for gaining the data required, theses check list designed by apparently  in diagnosing research dimensions and measurem

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Publication Date
Thu Mar 31 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetics and Mass Transfer Study of Oleic Acid Esterification over Prepared Nanoporous HY zeolite
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A mathematical model was proposed to study the microkinetics of esterification reaction of oleic acid with ethanol over prepared HY zeolite catalyst. The catalyst was prepared from Iraqi kaolin source and its properties were characterized by different techniques. The esterification was done under different temperature (40 to 70˚C) with 6:1 for molar ratio of ethanol to oleic acid and 5 % catalyst loading.

   The microkinetics study was done over two period of time each period was examined individually to calculate the reaction rate constant and activation energy. The impact of the mass transfer resistance to the reactant was also investigated; two different studies have been accomplished to do this purpose.

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Publication Date
Wed Mar 30 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Kinetics and Mass Transfer Study of Oleic Acid Esterification over Prepared Nanoporous HY zeolite
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A mathematical model was proposed to study the microkinetics of esterification reaction of oleic acid with ethanol over prepared HY zeolite catalyst. The catalyst was prepared from Iraqi kaolin source and its properties were characterized by different techniques. The esterification was done under different temperature (40 to 70˚C) with 6:1 for molar ratio of ethanol to oleic acid and 5 % catalyst loading.    The microkinetics study was done over two period of time each period was examined individually to calculate the reaction rate constant and activation energy. The impact of the mass transfer resistance to the reactant was also investigated; two different studies have been accomplished to do this purpose.    The e

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Publication Date
Wed Jun 01 2022
Journal Name
Journal Of The College Of Languages (jcl)
A comparative study of the pivotal characters in the novel "Al-Shahz" and the script "Hamoon": بررسی تطبیقی شخصیت¬های محوری در رمان «الشحّاذ» و فیلم‌نامۀ «هامون»
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The novel is the revelation of the attitudes of every age. And the writers do not know the winner of their stroke to express these events، The research has been working on a descriptive-analytical approach based on the American Comparative School، Al-Shahez's novel explores the work of the nobly and the film by Hamoun by Dariush Mehrjui By relying on the main characters of these two narratives, they depict a picture of Egypt and Iran From the symbolic lines of these works. In fact, the authors of this research have tried to initiate the introduction and analysis of these two works In fact, the authors of this research have tried to initiate the introduction and analysis of these two works.

 The results of the research show that

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Publication Date
Thu Jan 06 2022
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of an Instructional Program on Patientsꞌ Knowledge about Home Safety While Receiving Anti -Cancer Medications at Al- Karama Teaching Hospital in Al-Kut City
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Objectives: To determine the effectiveness of the instructional program on patients’ knowledge about home safety while receiving anti-cancer treatment at  Al- Karama Teaching Hospital in Al-Kut City.

Methodology:   A quasi-experimental design is conducted through the application of a pre-test and post-test approach for the study and control groups from February 5th, 2020 to April 25th, 2020. A non–probability (purposive) sample of (50) patients treated at the Blood Disease and Oncology Center is selected and divided into two groups. Each group contains (25) patients as control and study groups. An instrument is constructed that is comprised of two parts; t

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