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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
Mon Jun 01 2009
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of performance of some industrial companies In the default reference comparison method Field study in the public companies of cement (Iraqi - North - South
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The increasing Global Competitive and the continuous improvement in information technology has led the way to the development of the modern systems and using modern techniques. One of these techniques is benchmarking style and Total Quality Management all of them are used to improve the production process and target rid from the losts on the other side.

The Benchmarking style has become a very important for all the industrial systems and the serving systems as well. And an instrument to improve their performance specially those which are suffering from the highness of the costs or waste in time on the other side.

This study aims to depend on virtual Benchmarking style in the eval

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Publication Date
Sat Sep 01 2018
Journal Name
Journal Of Interdisciplinary Nanomedicine
Evaluation of intraductal delivery of poly(ethylene glycol)‐doxorubicin conjugate nanocarriers for the treatment of ductal carcinoma in situ (DCIS)‐like lesions in rats
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Abstract<p>Ductal carcinoma in situ is the most commonly diagnosed early stage breast cancer. The efficacy of intraductally delivered poly(ethylene glycol)‐doxorubicin (PEG‐DOX) nanocarriers, composed of one or more DOX conjugated to various PEG polymers, was investigated in an orthotopic ductal carcinoma in situ‐like rat model. In vitro cytotoxicity was evaluated against 13762 Mat B III cells using MTT assay. The orthotopic model was developed by inoculating cancer cells into mammary ducts of female Fischer 344 retired breeder rats. The ductal retention and in vivo antitumour efficacy of two of the six nanocarriers (5 kDa PEG‐DOX and 40 kDa PEG‐(DOX)<sub>4</sub>) were investigated based o</p> ... Show More
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Publication Date
Sun Oct 21 2018
Journal Name
Al-kindy College Medical Journal
Evaluation of the clinical examination in thediagnosis of acute medial collateral ligament injury of the knee joint in comparism with examination under general anesthesia
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Background: Tear of MCL of the knee is a frequent problem among knee ligaments injuries.Injuries to the MCL are usually caused by contact on the outside of the knee and are accompanied by sharp pain on the inside of the knee. Contrary to most other knee ligaments the medial collateral ligament (MCL) has an excellent ability to heal, being fairly large and well vascularised structure. The vast majority of isolated medial ligament injuries heal without significant long-term problems

Objectives: is to compare between the early clinical examination, and assessment under general anesthesia (GA), and to find out the best methods to assess the MCL tear especially in suspected cases.

Type

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Publication Date
Thu Nov 01 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of the performance of private hospitals from the point of view of the beneficiaries (A field Study in the private Sector hospitals in Baghdad)
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Objectives: This Paper is an attempt to evaluate the services provided by the private hospitals
and to identify the strength and weakness in
their performance The results can be utilized in stating conclusion and recommendations to improve
and activate the role of private medical sector in society .
Methodology: A questionnaire has be designed for this purpose and distributed to ( 132 ) beneficiaries
mostly from Baghdad private hospitals .
Results: The paper has come out with many important results . Among These are the following :
* these who benefit from services provided by private hospitals believe that the good performance of
such hospital is not due to the medical services alone but also to scientific aspect

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Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Synthesis of Carbon Nanotubes Using Modified Hummers Method for Cathode Electrodes in Dye-Sensitized Solar Cell
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      In this research, carbon nanotubes (CNTs) is prepared  through the Hummers method with a slight change in some of the work steps, thus, a new method has been created for preparing carbon nanotubes which is similar to the original Hummers method that is used to prepare graphene oxide. Then, the suspension carbon nanotubes is transferred to a simple electrode position platform consisting of two electrodes and the cell body for the coating and reduction of the carbon nanotubes on ITO glass which represents the cathode electrode while platinum represents the anode electrode. The deposited layer of carbon nanotubes is examined through the scanning electron microscope technique (SEM), and the images throughout the research show the

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Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
Semantic functions of repetitive synthesis in Adnan al-Sayegh's poetry: زينب دريانورد - رسول بلاوي - علي خضري
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The art of synthesis is one of the most important pillars in cinematic art, as the director combines cinematic shots to produce a third shot in the mind of the recipient by various methods such as mental synthesis, analogous synthesis, rhythm synthesis, parallel synthesis and repetitive synthesis, Repetitive synthesis is one of the most important techniques in cinematic montage. Through repetitive synthesis, the director is able to link the shots and scenes with each other, and this is what we see in the poetic imagery of Adnan Al-Sayegh when he links the visual images to each other, especially those images that manifest the manifestations of grief and misery following the misfortunes that befell in His homeland. This study follows the d

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Publication Date
Thu Jan 23 2025
Journal Name
Научный форум
PHRASEOLOGISMS RELATED TO THE USE OF COLORS IN SPEECH AS A MEANS OF ENRICHING MODERN RUSSIAN LANGUAGE
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The paper examines key aspects of the use of phraseologi-cal units related to colors in Russian culture and speech. It explores their role in shaping cultural identity, reflecting national characteristics and men-tality. The study analyzes the frequency and contexts of the use of color-related phraseological units in contemporary speech, as well as the influ-ence of media and literature on their popularization. The author highlights the significance of phraseological units in preserving cultural heritage and fostering a deeper understanding of language and culture.

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Publication Date
Wed Mar 29 2023
Journal Name
Journal Of The College Of Education For Women
A Cognitive Linguistic Study of Visual Language as a Reflection of Culture: Violence Against Women in Iraq
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The present work is qualitative descriptive. It aims to examine the idiosyncratic schema when deciphering the selected violence-based panel from Nasser Ibrahim’s caricatures. The researchers accordingly adopted part of Sharifian’s (2011) Cultural Schema model, particularly that part that is concerned with the examining the micro/idiosyncratic level of understanding. The study has revealed that the participants have not only differed among themselves regarding the way a figure is being denotatively conceptualized, they also highlighted different exact conceptualizations for the same figure, such as: using various adjectives that reflect various levels of intensity, emphasizing the behavioral aspect or the appearance of the figure, ado

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Publication Date
Tue Mar 22 2022
Journal Name
Journal Of The College Of Basic Education
Directing treatment of the concept of cruelty in the Iraqi theater show (Autumn play as a specimen)
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    رافقت القسوة الانسان منذ القدم  وكثيرا ما تم الخلط بينها وبين العنف لشدة التقارب بينهما , وهنا يحاول البحث  ان يفصل بين كلا المفهومين ويتفرد بمفهوم القسوة, الذي سلط عليه الضوء في المسرح لأول مرة على يد الفرنسي(انطوان ارتو)  في محاولة للكشف عن المعالجة الاخراجية التي قدمها المخرج العراقي(صميم حسب الله) لمفهوم القسوة في مسرحيته الموسومة (خريف) ويتضمن البحث نبذه  (مفهوم القسوة في الفكر الانساني) وكذلك (الق

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Publication Date
Sat Jul 18 2020
Journal Name
College Of Islamic Sciences
Methodology of Bible Criticism of Muslim Scholars in South Africa Ali Safraz Khan Gumal as a sample
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This paper and research paper analyzes the critical methodology of "Ali Khan Joommal “ about the Bible , directed in most of the textual criticism of the Torah, and its highest criticism is directed to both the Old and New Testaments.

Joommal  was distinguished by the mental methods and examples accompanying his era, while maintaining the general context in which Muslim scholars had previously followed, and he was distinguished from them by his many citations to the Western literature of Jews or Christians, in short it is a critical phenomenon worthy of study and evaluation.

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