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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
Wed Dec 29 2021
Journal Name
Journal Of The College Of Education For Women
The Skills of Intended Meaning behind the Context when Reading Poetry among Fifth Grade Students- Literary Branch from Teachers’ Perspectives
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        The current research aims to investigate the skills of the intended meaning beyond the context when reading poetry among fifth literary students. To achieve the aim of the research, the researcher has followed the descriptive approach and used two tools: an open questionnaire that includes an inquiry about the skills of the intended meaning beyond the poetic context, and a closed questionnaire that were examined by the juries, and modified accordingly. Besides, its validity and stability were examined by applying the study on an exploratory sample of (15) teachers to reach its final version and determine the time required to answer it. Then, the researcher applied it on the research sample of (9

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Publication Date
Sun Dec 15 2019
Journal Name
Al-academy
The Effect of The Illustration Program on Fashion Design Inspired by Historical Costumes: تهاني ناصر العجاجي -هدى عبد العزيز المقرن
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This research aims to identify the role and impact of illustrations in contemporary fashion design inspired by historical costumes. Historical fashion aesthetics are adapted to design drawings. The experimental method was followed and a sample of 31 students in the department of fashion and textile design, third level were selected. Each student carried out two original historical and contemporary design. The models were executed two times: one with the usage of the program and the other without program help. The tools that were used are the program, the scale, the pre-skill test, and the post-skill test. One of the most relevant results of the research is the possibility of using historical costumes to highlight creativity and innovatio

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Publication Date
Mon Feb 13 2023
Journal Name
Journal Of Educational And Psychological Researches
A Proposed Strategy to Develop Postgraduate Studies at King Khalid University to Support the Achievement of the Kingdom's 2030 Vision
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Abstract

The aim of this research is to formulate a proposed strategy for developing graduate studies at King Khalid University to support the achievement of the Kingdom's vision (2030). The research used the descriptive survey approach. The research community consisted of all graduate students at King Khalid University. The research was conducted on a random sample included (623) Male and female students, this research relied on the questionnaire as the main tool for collecting its data. The results revealed that the research sample believes that all the proposals included in this research are very important for the development of postgraduate studies at King Khalid University to support the achievement of the K

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Publication Date
Sun Jun 30 2024
Journal Name
Anbar Journal Of Agricultural Sciences
THE GENETIC DIAGNOSIS OF THE BACTERIA ISOLATED FROM THE AGRICULTURAL SOIL SUSTAINED FARMS BY THE POLYMERASE CHAIN REACTION TECHNIQUE QPCR
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The measurements and tests of the samples conducted in the laboratories of the College of Agriculture included isolating bio-fertilizers and testing the efficiency of isolates that fix atmospheric nitrogen and solubilize phosphorous compounds. Bacteria were isolated and identified from the rhizosphere soils of different plants collected from various agricultural areas. A total of 74 bacterial isolates were obtained based on the phenotypic characteristics of the developing colonies, as well as biochemical and microscopic traits. The results of isolation and identification showed that among the 74 bacterial isolates, there were 15 isolates of A. chroococcum, 13 of Az. lipoferum, 13 of B. megaterium, 10 of P. putida, 10 of Actinomycetes, and n

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Preparation, Characterization & Biological activity for Some Iron(II) Complexes Containing Mixed Ligands (Benzilazine & Semicarbazone) & Study of Laser Effect on Them
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The research included preparation of new iron(II) complexes with mixed ligands including benzilazine(BA) and semicarbazone ligands {benzilsemicarbazone- BSCH or benzilbis(semicarba-zone)- BBSCH2 or salicylaldehydesemicarbazone- SSCH2 or benzoinsemicarbazone- B'SCH2}.by classical and microwave methods. The resulted complexes have been characterized using chemical and physical methods. The study suggested that the above ligands form ionic complexes having formulae [Fe(SCHi)(BA)(Cl)m](Cl)2-m {where SCH, BSCH, BBSCH2, SSCH¬2 or B'SCH2 ligands; m=1 or 2}. Hexacoordinated mononuclear complexes have been investigated by this study and having octahedral geometries. The effect of laser ray type visible region have been studied on solid ligands and

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Publication Date
Tue Mar 04 2008
Journal Name
Journal Of Baghdad College Of Dentistry
Twelve months clinical comparison between modified Widman flap with or without enamel matrix derivative for the treatment of infrabony defects
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Publication Date
Mon Oct 01 2018
Journal Name
International Journal Of Biosciences
Detection of Escherichia coli O157 H7 isolated from infected dogs with urinary tract infections using real time - polymerase chain reaction
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Publication Date
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Numerical Solutions for the Nonlinear PDEs of Fractional Order by Using a New Double Integral Transform with Variational Iteration Method
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This paper considers a new Double Integral transform called Double Sumudu-Elzaki transform DSET. The combining of the DSET with a semi-analytical method, namely the variational iteration method DSETVIM, to arrive numerical solution of nonlinear PDEs of Fractional Order derivatives. The proposed dual method property decreases the number of calculations required, so combining these two methods leads to calculating the solution's speed. The suggested technique is tested on four problems. The results demonstrated that solving these types of equations using the DSETVIM was more advantageous and efficient

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Publication Date
Fri Oct 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
Institutional Performance Assessment using a model of the European Foundation for Quality Management (EFQM) A case study at an organization
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The study aims to use the European Excellence Model (EFQM) in assessing the institutional performance of the National Center for Administrative Development and Information Technology in order to determine the gap between the actual reality of the performance of the Center and the standards adopted in the model, in order to know the extent to which the Center seeks to achieve excellence in performance to improve the level of services provided and the adoption of methods Modern and contemporary management in the evaluation of its institutional performance.

The problem of the study was the absence of an institutional performance evaluation system at the centre whereby weaknesses (areas of improvement) and st

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Publication Date
Fri Jun 30 2023
Journal Name
International Journal Of Intelligent Engineering And Systems
DeepFake Detection Improvement for Images Based on a Proposed Method for Local Binary Pattern of the Multiple-Channel Color Space
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DeepFake is a concern for celebrities and everyone because it is simple to create. DeepFake images, especially high-quality ones, are difficult to detect using people, local descriptors, and current approaches. On the other hand, video manipulation detection is more accessible than an image, which many state-of-the-art systems offer. Moreover, the detection of video manipulation depends entirely on its detection through images. Many worked on DeepFake detection in images, but they had complex mathematical calculations in preprocessing steps, and many limitations, including that the face must be in front, the eyes have to be open, and the mouth should be open with the appearance of teeth, etc. Also, the accuracy of their counterfeit detectio

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