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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
Tue Feb 19 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The role of Islamic banks to attract savings to funding banking activities in Iraq For period (2008-2012)
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Islamic banks are a financial institution that is interested in attracting financial savings from financial entities and directing them towards those with financial deficits, both for consumption purposes or for investment purposes. It provides banking services provided by commercial banks and other services But based on the principles and principles of Islamic law, and because of its recent emergence in Iraq, its ability to attract savings is not like non-Islamic commercial banks, which puts them in the option of using their capital to achieve its objective of banking. The research started from the premise that "Islamic banks in Iraq during the period (2008-2012) rely on their capital to perform their activities more than they rely on d

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Publication Date
Wed Apr 06 2022
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Management using the Six Sigma approach to cost rationalization of activities : Application in the Iraqi mechanical carpet factory
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The textile industries play a prominent role in reviving the national economy, but they are currently suffering from several problems, including the high costs of their activities, the low quality of their production processes, and accordingly, the hexagonal diffraction approach came to help analyze production activities to determine which of them are the most expensive and do not have a benefit or cost greater than Its benefit as a result of waste and losses that accompany its implementation. And by applying to the Iraqi mechanical carpet factory, the research reached several conclusions, the most important of which is the presence of several sources of waste and loss, such as activities and operations that do not add value, whi

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Publication Date
Sat Jul 31 2021
Journal Name
Iraqi Journal Of Science
Effects of Caper (Capparis Spinosa) and Acetic Acid on Lipid Profile and Protein Concentration in the Serum of Albino Mice
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     This study aimed to determine the effects of alcoholic and aqueous extracts of caper (Capparis Spinosa) and acetic acid on serum lipid profile and proteins levels in mice.  Sixty adult mice with an average weight of 24±4 g grams were divided into four groups (15 mice for each). The first group (G1) was administrated daily with an oral dose of caper alcoholic extract (200 mg/kg) for 28 days. The second group (G2) was administrated daily with an oral dose of caper aqueous extract (200 mg/kg) for 28 days. The third group (G3) was administrated with a daily dose of 10 % acetic acid  (2 ml/kg) for 28 days. The fourth Group (G4) was administrated daily with distilled water for 28 days, as a control

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Publication Date
Sat Mar 18 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Role of Salsylic Acid, Fertilizer NPKzn and Sodium Chloride and Theris interactions in Some Morphological Parameters of Allium cepa L.
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 The experiment was condncted in greenhouse of Botanical Garden at Biology Garden Dept,College of Education for Pure Science (Ibn-Al-Haitham),University of Baghdad , during the growing season  2013-2014 to study the role of salcylic acid in three concentrations (0.12and24) ppm and two levels of NPKZn fertilizer ( 0. 160) kg.H‾1 and four concentrations of sodium chloride (0.50.100and150) Mmol and the intreaction between salcylic acid and NPKZn on some of morphological parameters of Allium cepa.                                 The experiment was performed with random compelete block design (RCBD)with three replications and the results showed the

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Publication Date
Tue Jan 11 2022
Journal Name
Journal Of Research In Medical And Dental Science | Vol. 10 | Issue 1 | January-2022
Esthetic Improvements of Various Degrees of White Spot Lesion Using Resin Infiltration and Micro-Abrasion (An In Vitro Study)
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Background: White spot lesions are esthetic problems caused by subsurface enamel demineralization that seen as white opacity. Aim of the study: This study aimed to evaluate and to compare the color change after the treatment of the white spot lesions with resin ‹nϔ‹Žtrƒt‹on and micro abrasion. Materials and Methods: rt‹ϔ‹…‹ƒŽ white spot lesions were generated on 48 premolar teeth by the use of a demineralization solution. The teeth were randomly divided using the Diagnodent into three study groups (16 teeth for each group) depending on the depth of the induced lesions: outer enamel, inner enamel and outer dentine. Then each group was fatherly subdivided into two groups (8 teeth for each group) the ϔ‹rst group was treated wit

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of Tea Tree, Thymus Vulgaris and Nigella Sativa Oils on The Elimination of Enterococcus Faecalis (In Vitro Study)
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ABSTRACT Background: The main goal of chemomechanical endodontic treatment is the reduction or elimination of microorganisms from root canal system. The intracanal medicaments were used to enhance the disinfection process. This study was conducted to evaluate the antibacterial effect of thymus vulgaris, tea tree essential oils and cold pressed black seed oil (BSO) against E.faecalis. Materials and methods: E.faecalis was isolated from ten patients in need for endodontic treatment. The sensitivity of E.faecalis to the tested oils was evaluated in different concentrations in agar well diffusion method and compared with calcium hydroxide. The sensitivity of E.faecalis to vapor of the tested oils was also evaluated, in disk vaporization method

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Publication Date
Tue Mar 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of Resin Infiltration and Microabrasion on the Microhardness of the Artificial White Spot Lesions (An in Vitro Study)
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Background: White spot lesion is the first visible sign of dental caries that is characterized by demineralized lesion underneath an intact surface. Several studies demonstrated that they could be treated using noninvasive techniques like the use of fluoride or casein phospho-peptide and amorphous calcium phosphate. Improvement in aesthetic outcomes by covering the demineralized enamel is one of the advantages of the use of resin infiltration and opal-ustre microabrasion, which are two new techniques that had been used for treatment of white spot lesion. The purpose of this study was to evaluate the impact of resin infiltration and microabrasion in the microhardness of the artificial white spot lesions at various depths. Material and method

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Publication Date
Tue Mar 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of Resin Infiltration and Microabrasion on the Microhardness of the Artificial White Spot Lesions (An in Vitro Study)
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Publication Date
Tue Feb 04 2025
Journal Name
Journal Of Baghdad College Of Dentistry
The Influence of Caries Infiltrant Combined with and without Conventional Adhesives on Sealing of Sound Enamel (In Vitro Study)
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Background: The formation of white spot lesions around fixed orthodontic attachments is a common complication during and after fixed orthodontic treatment, which hinders the result of a successfully completed orthodontic treatment. The aim of the study was to assess the effectiveness of the Caries Infiltrant (ICON®) on prevention of caries on the smooth enamel surface when applied alone or combined with conventional adhesives. Materials and methods: Seventy eight human premolar enamel discs were randomly assigned to six groups (n=13). The discs were etched and treated with resins of different monomer content forming the following groups: (1)Untreated etched samples served as the negative control, (2) ICON® (DMG), (3) Adper™ S

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Publication Date
Sun Jan 01 2023
Journal Name
The Egyptian Journal Of Hospital Medicine
Assessment of Plasma Jet Therapy of Tooth Root Canal Infected with Escherichia Coli and Enterococcus Faecalis Biofilm In Vitro
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Background: Common and persistent isolate ina the teeth following failed therapy of the root canal is the gram-positive facultative bacterium Enterococcus faecalis and Escherichia coli, which develop biofilm through a complicated process that results in the formation of a biofilm. Enterococcus faecalis and Escherichia coli are significant factors that cause chronic periradicular lesions after root canal therapy. Aim: This study aimed to treat the root canal tooth infected with Escherichia coli and Enterococcus faecalis Methods: In this study biofilm formation was done for Escherichia coli in growth phase cultured in a brain heart broth Enterococcus faecalis and Escherichia coli cultured in Luria-Bertani (LB) infusion medium for 18 hrs. Then

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