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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 Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Effect of Acetic Acid on Electrochemical Behavior of Sealed AA2319-T3 Al-Alloys Anodized in Phosphoric Acid Electrolytes
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Abstract

      The present study investigates the effect of acetic acid on corrosion behavior and its potential of hydrothermally sealed anodized AA2319-Al-alloys. Anodizing treatment was performed in stagnant phosphoric acid electrolyte with or without addition of acetic acid. Hydrothermal sealing was carried out in boiling water for each anodized specimen. The open circuit potential of the unsealed and sealed anodized samples was examined using open circuit potential measurement for the purpose of starting in scanning polarization diagrams. The potentiostatic polarization technique measurements were performed to assess corrosion behavior and sealing quality (i.e., degree of sealing) of

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Publication Date
Sun Apr 07 2013
Journal Name
Journal Of Educational And Psychological Researches
Effectiveness of enrichment activities through using software program for second graders in Conversation article
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Today we are witnessing huge scientific and technical progress so we need more skills and methods of thinking that needs to be acquired by the teacher, as the importance of computers in education  there are  many teachers  suffering  of the difficulty in teaching for pupils . researchers tried to  find a good suitable way with the technological  interests for now which represent by  computer design software and the introduction of enrichment activities in the curriculum because it is one of a contemporary trends for the development of the Arabic language with various levels of education and knowing if this program has negative or positive impact.

So&nbsp

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Publication Date
Sun Oct 21 2018
Journal Name
Al–bahith Al–a'alami
Ways to face rumors in the social networking site Facebook: Research thesis from the PhD thesis
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The research deals with the subject of «ways to face rumors in the site of social networking Facebook», a research based on a doctoral thesis, as the research dealt with rumors in the most dangerous type of new media, which sites of social communication with the global community as spreading rumors of all kinds and afflicts everyone who has eyes on him Of the audience of these sites, and aims to identify the rumors on Facebook because it is one of the most popular sites in the world and the strategy of combating the rumors published by Facebook users in their personal pages and groups that organize them, as well as identify methods and methods that can be During which the face of the rumors in the said site and eliminate them t

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Crossref
Publication Date
Thu Nov 20 2025
Journal Name
Al–bahith Al–a'alami
Evaluation of the Iraqi Community for Election Campaigns for Candidates of the House of Representatives and Media Coverage in March 2010: (Cairo as a Model)
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The elections of the Council of Representatives in Iraq are one of the manifestations of political participation, which makes it attracts the attention of researchers. Where Iraq witnessed in 2005 important political events in the Iraqi arena, a pluralist parliamentary elections or elections in Iraq by direct free election on January 30, the first almost half a century ago. On November 15 of the same year, Iraq adopted a permanent constitution for the country through a popular referendum.

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Crossref
Publication Date
Wed Nov 02 2022
Journal Name
Res Militaris
Cultural Activities The Iraqi Ministry of Culture, Tourism and Antiquilies
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It’s an attempt to identify the cultural activities of the Ministry of Culture, Tourism and Antiquities, which are provided by the Ministry of Culture, Tourism and Antiquities and the departments affiliated with the Ministry of Culture only, not tourism and antiquities. The most important results areIs that the Ministry of Culture, Tourism and Antiquities has many cultural activities such as (festivals, exhibitions, conferences, fashion shows, concerts, musical evenings, theatrical and cinematic performances) in addition to literary series and cultural magazines, which are directed to the public in general, whether it is elite or not, and this shows the extent The importance of cultural activities published by the Ministry of Culture, Tou

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Publication Date
Mon Jul 03 2023
Journal Name
Journal Of Polymer & Composites
Metal Complexes of Cephalexin and Their Biological Activities: A Review
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Cephalexin and its derivatives are commonly utilized in the pharmaceutical and medicinal industry due to their biological and pharmaceutical activities, including anti-microbial, anti-cancer, anti-bacterial, and herbicidal activities as well as possessing high palatability and being useful for skin and joint infections. Interestingly, some organic drugs, including cephalexin, which exhibit toxicological and pharmacological properties, can be administered in forms of metal complexes. Many researchers have synthesized organic ligands derived from cephalexin in forms of Schiff bases and azo compounds which exhibited higher biological and medicinal properties when compared to cephalexin alone. One of the important features that make Schiff base

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Publication Date
Sat Jan 31 2015
Journal Name
Journal Of Al-qadisiyah For Pure Science
synthesis ,spectral studies and antimicrobial evalution of 6,6-(1,2-benzenediazo)bis(3-amino benzoic acid) complexes with some metal ions
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Publication Date
Thu Nov 20 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Propolis from Kurdistan region as a new resinous sealer in root canal obturation-part I biocompatibility study
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Background: Many materials were proposed as root canal obturating materials but the biocompatibility issue remains to be a critical one. Propolis has been used as a therapeutic agent since the time of Hippocrates. It is known that propolis exhibits some pharmacological activities, such as antibacterial, antiviral, antifungal and anti inflammatory activity. Materials and methods: Eighteen albino rats were used in the study and divided randomly into three groups of 6 animals for each group. Each group was scheduled to be sacrificed at different time periods, which were three days, one week and three weeks. Propolis and ZOE sealer implants of 4mm in diameter and 0.5 gm in weight were implanted in the dorsal side of the rats. At the end of the

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Publication Date
Thu Apr 14 2016
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
Study The Effect of α-amylase Inhibitors Isolated from Plant Sources on Some Mold.: Study The Effect of α-amylase Inhibitors Isolated from Plant Sources on Some Mold.
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Activity test of the inhibitors purified from barley and broad beans crop proved the inhibition activity against 6 types of rots Pencillium ssp and Aspergellusflavus and Aspergillus niger and Fusarium solani and Fusarium semitectum and Mucor with three concentrations 0.1 and 0.2 and 0.3 mg/ml, where the inhibitor purified from the second peak of broad beans proved that it had a higher inhibition activity against the growth of test rots which were 53.75 and 62.5 and 78.5 and 76.25 and 84 and 18.8% respectively, at 0.3 mg/ ml followed by the first peak of the inhibitor purified from broad beans the inhibition activity were 43.75 and 50 and 62.96 and 75 and 80 and 12.5 then the inhibitor purified from barley in which the inhibition activity

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Publication Date
Thu Nov 20 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of shear bond strength between thermosens as relining material and different denture base materials
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Background: Denture relining is the process of resurfacing of the tissue side of the ill fitting denture, the bond strength at the relining-denture base interface is most important for denture durability.The aim of present study was to evaluate the shear bond strength between the thermosens as relining material and different denture base materials that bonded by thermo fusing liquid. As this corrective procedureis the common chair side procedure in the dental clinic. Material and method: Sixty samples were prepared and divided into three main groups according to the type of denture base materials.Group (A) referred to the heat cure acrylic samples which consisted of 20 samples. Group (B) referred to the high impact acrylic samples which con

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