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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
Sun Mar 26 2023
Journal Name
Wasit Journal Of Pure Sciences
Covid-19 Prediction using Machine Learning Methods: An Article Review
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The COVID-19 pandemic has necessitated new methods for controlling the spread of the virus, and machine learning (ML) holds promise in this regard. Our study aims to explore the latest ML algorithms utilized for COVID-19 prediction, with a focus on their potential to optimize decision-making and resource allocation during peak periods of the pandemic. Our review stands out from others as it concentrates primarily on ML methods for disease prediction.To conduct this scoping review, we performed a Google Scholar literature search using "COVID-19," "prediction," and "machine learning" as keywords, with a custom range from 2020 to 2022. Of the 99 articles that were screened for eligibility, we selected 20 for the final review.Our system

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Computer Assisted Immunohistochemical Score Prediction Via Simplified Image Acquisition Technique
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Background: techniques of image analysis have been used extensively to minimize interobserver variation of immunohistochemical scoring, yet; image acquisition procedures are often demanding, expensive and laborious. This study aims to assess the validity of image analysis to predict human observer’s score with a simplified image acquisition technique. Materials and methods: formalin fixed- paraffin embedded tissue sections for ameloblastomas and basal cell carcinomas were immunohistochemically stained with monoclonal antibodies to MMP-2 and MMP-9. The extent of antibody positivity was quantified using Imagej® based application on low power photomicrographs obtained with a conventional camera. Results of the software were employed

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Publication Date
Sun Jan 01 2023
Journal Name
Computers, Materials & Continua
Hybrid Deep Learning Enabled Load Prediction for Energy Storage Systems
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Publication Date
Sun Jun 01 2014
Journal Name
Alustath Journal For Human And Social Sciences
Obstacles to the application of electronic management in university libraries: the universities of Baghdad and Al-Mustansiriya as a model.
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The research aims to identify the obstacles facing the application of electronic management in our university libraries, including the central library of the University of Baghdad and the central library of Al-Mustansiriya University, the research sample, as they are among the main libraries that used electronic technologies in managing some of their work and in providing their services, and they have a website via the Internet. The research relied on the case study method to identify the obstacles by visiting the two libraries, interviewing their managers and employees responsible for the departments, and answering inquiries about the obstacles that prevent the application of electronic management in order to identify them and find appropr

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Publication Date
Thu Oct 01 2015
Journal Name
Journal Of Educational And Psychological Researches
Anxiety of death among pregnant women in the light of some Demographic variables Governorates Bethlehem and Tulkarm as a model
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This study aims to identify the anxiety pregnant women have of dying, in the light of some Demographic variables in Bethlehem (age, residence, and the mother's job). The descriptive method was used in this study. To achieve the study purposes, the researchers developed a questionnaire as a tool of study, which consisted of (19) paragraphs ,after been verified of its validity & stability.

The researchers distributed questionnaires, and then analyzed them. Results illustrated that the levels of anxiety pregnant women in Bethlehem had of dying was average,  with a mean total score of (3.11),  and with a standard deviation that had the total score of (0.476). Results also illustrated statistical differences in the pregn

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Determination of Testosterone level as predictor for insulin resistance in young men with family history of type2 diabetes and hypertension.
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Background: Insulin resistance is associated with metabolic syndrome , type 2 diabetes and representing a risk factor for cardiovascular disease . This relationship may be modulated to some extent by age related changes in sex hormone status.. In particular, reduced total testosterone (TT) levels have been associated with insulin resistance and subsequent risk for developing type 2 diabetes. Aim of study: we examined whether low total testosterone level were associated with insulin resistance in young adult men. Methods: a total of 83 men (young adult men) divided into 2 group : (group1 ) 49 men with a risk factor for insu

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Publication Date
Thu Jun 06 2024
Journal Name
Bulletin Of The Iraqi Natural History Meseum
Morphological and molecular study of three species of Acrobeloides (Cobb, 1924) Thorn, 1937(Rhabdida, Cephalobidae) as new record in Iraq
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Publication Date
Wed Jul 01 2020
Journal Name
Journal Of Environmental Engineering
Sustainable Use of Concrete Demolition Waste as Reactive Material in Permeable Barrier for Remediation of Groundwater: Batch and Continuous Study
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Publication Date
Sun Nov 01 2015
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
Clinical and biochemical evaluation of facial acanthosis nigricans
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KE Sharquie, AA Noaimi, HG Mahmood, SM Al-Ogaily, Journal of Cosmetics, Dermatological Sciences and Applications, 2015 - Cited by 6

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Publication Date
Sat Apr 20 2019
Journal Name
Drug Invention Today
Preparation and evaluation of lornoxicam film-forming gel
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