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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 Jan 30 2019
Journal Name
Journal Of The College Of Education For Women
The Difficulties which Face Public Basic School Principals in Jarash Governorate in Editing Formal Letters and Correspondence and Means of Dealing With These Problems as Perceived by Them
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This study aimed at identity baying the difficulties which face public basic school
principals in jar ash governorate in editing formal letters and correspondence and means of
debating with these problems to collect data the researchers developed a question air were
established the population of the study which represents its sample consisted of 129 principals
65 males and 64 females
The results of the study revealed that the principals face difficulties in office and file
management in preparing plans and reports and writing formal letters and answering them
saved recommendations were presented among which were organizing training sessions and
workshops to train the principals on how to dead with there problems.<

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Publication Date
Mon Apr 10 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Domperidone Nanoemulsions for Oral Rout
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          The aim of the present study is to formulate, evaluate and characterize the nanoemulsion of Domperidone a poorly water-soluble anti-emetic drug.

           Domperidone powder is white or almost white powder, photosensitive, practically insoluble in water, slightly soluble in ethanol and in methanol; soluble in dimethylformamide. It is used as an antiemetic for the short-term treatment of nausea and vomiting of various etiologies.

           Solubility studies were conducted to select the oil, surfactant and cosurfactant. Phase diagrams were constructed by aqueous phase

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Publication Date
Mon Dec 20 2021
Journal Name
Baghdad Science Journal
Evaluation Method of Mesh Protocol over ESP32 and ESP8266
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Internet of Things (IoT) is one of the newest matters in both industry and academia of the communication engineering world. On the other hand, wireless mesh networks, a network topology that has been debate for decades that haven’t been put into use in great scale, can make a transformation when it arises to the network in the IoT world nowadays. A Mesh IoT network is a local network architecture in which linked devices cooperate and route data using a specified protocol. Typically, IoT devices exchange sensor data by connecting to an IoT gateway. However, there are certain limitations if it involves to large number of sensors and the data that should be received is difficult to analyze. The aim of the work here is to implement a self-

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Publication Date
Sun Feb 28 2021
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of Educational Performance according to Centralization and Decentralization
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The research aims to identify the effect of applying administrative decentralization to an educational performance by assessing educational performance before and after the process of transferring powers from the federal government (the Iraqi Ministry of Education) to local governments (governorates) as well as identifying the appropriate central or decentralized administrative system to advance the educational reality and performance. To achieve the goal of the research, educational data was collected and analyzed, as well as the measurement of educational performance indicators and analysis during two phases, the first represents the stage of applying the central system and spanned between the academic year (2011-2012) and the

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Publication Date
Fri Mar 30 2012
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Production and Evaluation of Biodiesel from Sheep Fats Waste
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Animal fats are a good, promising and ethical alternative source for biodiesel production, but they need more complex treatments than vegetable oils. Iraqi butchery plants waste fats (sheep fat) which are suggested as feedstock to produce biodiesel. This type of fat contains a large quantity of free fatty acids (FFAs) (acid number 49.13 mg KOH/g of fat). The direct transesterification of such fats produce high amount of soap instead of desired biodiesel, so a pre-treatment step (to reduce FFAs) is necessary before transesterification. This step was done by esterification of the free fatty acids in the fat by adding ethanol and using 1% acid catalyst (H2SO4) for 30 minutes. The results showed that the acid number of sheep fat after pre-tr

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Publication Date
Mon Nov 05 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation and Comparison of Complete Dentures’ Complaints: Post-insertion
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Aims: This study aims to compare patients’ complaints and problems of wearing complete dentures.
Methodology: The sample included 40 Iraqi patients who are wearing complete dentures from about five years ago. They
were selected randomly with a age range between (55–65) years. The questions asked to the patients were listed according
to the recent classification of post-insertion problems.
Result: The results showed that the percentage of patient's complaint from adaptation problems (62.1%) was higher than
looseness problems (61.3%) and discomfort problems (39.3%) as followed.
Recommendation: Dentists need thorough knowledge of anatomy, physiology, pathology and psychology. The assessing
of the psyche and emotions

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Publication Date
Tue Feb 01 2022
Journal Name
Journal Of Engineering
Evaluation and Development of the (Hilla – Daghara) Rivers System
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Shatt Al-Hilla branches from the left of Euphrates River, U/S Hindiyah Barrage, Iraq, and extends about 100 km. It branches at the end into Shatt Al-Diwaniya 112 km and Shatt Al-Daghara 64 km. The study aims to evaluate and develop (Hilla-Daghara) rivers system, which is included Shatt Al-Hilla and Shatt Al-Daghara. Fieldwork began from (26 October until December) 2020. M9, S5 devices, and the installed staff gauges were used to measure discharges and water levels, respectively. A one-dimensional model was developed for the study area by HEC-RAS, after calibration and verification by field measurements; the Manning's n of Shatt Al-Daghara is found to be 0.022. Five Scenarios were simulated to study the reach under the cu

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Publication Date
Fri Jun 07 2024
Journal Name
Medicine
Impact of TYMS gene polymorphism on the outcome of methotrexate treatment in a sample of Iraqi rheumatoid arthritis patients – identification of novel single nucleotide polymorphism: Cross-sectional study
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The current work aims to evaluate the association between genetic mutations in thymidylate synthetase (TYMS gene in exon1 and partial regions of promotor and intron 1 [877 bp, 657,220–658,096 bp]) and the therapeutic outcomes for rheumatoid arthritis (RA) Iraqi patients. An observational cross-sectional study involving 95 RA patients with established RA patients based on their methotrexate treatment responsiveness. Genetic sequencing of the TYMS gene was performed for all patients according to the instruction manuals of the sequencing company (Macrogen Inc. Geumchen, South Korea). Four polymorphisms were identified by sequencing 95 randomly selected patients in the noncoding region of TYMS

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Publication Date
Fri Jan 01 2021
Journal Name
Ieee Access
Total Dissolved Salt Prediction Using Neurocomputing Models: Case Study of Gypsum Soil Within Iraq Region
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Publication Date
Sun Sep 01 2024
Journal Name
Baghdad Science Journal
Isolation and Identification of Flavonoid Compounds from Euphorbia Milii Plant Cultivated in Iraq and Evaluation of its Genetic Effects on Two Types of Cancer Cell Line
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يعتبر "تاج الأشواك" أو نبات شوكة المسيح، وهو من نباتات الزينة الطبية ، ينتمي إلى جنس يوفوربيا. E. milii يحتوي كميات وفيرة من المركبات الفينولية ، التربينات، الستيرويدات والقلويدات. كانت الأهداف الرئيسية لهذه الدراسة هي فحص مستخلصات الفلافونويد والنانو فلافونويد ضد نوعين من خطوط الخلايا السرطانية. تم تصنيع مركبات الفلافونويد النانوية عن طريق تفاعل مركب الكيتوسان والماليك اسد. تم تحليل مركبات الفلافونويد ال

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