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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 Aug 15 2019
Journal Name
Scholarspace
Folklore as Resistance in Postcolonial Narratives and Cultural Practices: Hawaiian, African American, and Iraqi
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Colonialism radically transformed the cultures of colonized peoples, often rupturing Indigenous traditions and folklore. Whether creating colonial discourse, promoting orientalist literature, advocating western educational institutions, or through biased media representations, imperial powers systematically oppressed Indigenous and Native peoples. Subjugated communities, however, created, and still form postcolonial discourse from their knowledge systems. This discourse insists on Indigenous and Native culture as central to Indigenous and Native peoples identity. This study examines the postcolonial literature of three groups: Kānaka Maoli, African Americans, and Iraqis. The scope of this dissertation scrutinizes how folklore is employed

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Publication Date
Sat Jul 01 2023
Journal Name
Iop Conference Series: Earth And Environmental Science
Evaluation of Sustainable Spatial Suitability of Urban and Population Expansion in Al Hillah City Using Remote Sensing Techniques
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Abstract<p>The study focused on explaining urban expansion and sustainable development of urban land and explaining the role of population expansion in Al Hillah city, Al Hillah city in the center of Babylion Governorate located. The study relied on analyzing the population data of the city of Al Hillah for a period of time (22 years) for the period (2000-2022). This data was analyzed and its role in planning and designing residential areas and neighborhoods in the Al Hillah city was analyzed based on the standards of urban planning and sustainable growth of cities. Landsat 5TM was used in the investigation, Landsat 8OLI satellite data to retrieve the NDVI, NDBI, and NDWI. The findings showed th</p> ... Show More
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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Knowledge, Attitudes and Experience of off-label Drug Prescribing Practice among Physicians in Baghdad City Hospitals
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Abstract

The present study aims to assess the knowledge, attitude, and experience of off-label prescribing practice among physicians in Baghdad city hospitals. This cross-sectional study was performed through the period from November 1st 2018 to March 2019 at 17 hospitals, a self-administered questionnaire was utilized to collect data from the physicians, and the targeted hospitals were randomly selected at different regions in Baghdad City area. Out of the 400 distributed questionnaires to the physicians, 383 of them were returned completed, 57.2% indicated that they were reasonably familiar with the term “off label drug”, 57.7% mentioned that the most common medical reasons for the prescribing o

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Publication Date
Mon Jan 13 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The evaluation of the role of the information system in reducing tax evasion
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This research attempts to evaluate the role of the information system by highlighting its importance in providing date and information to the tax administration the process of tax accounting for those who are subject to income tax whether they are individuals or companies where the effective information system provides accurate and reliable information in a timely manner.

At the theoretical part of the research, the research approaches the problem of the research represented in that whether the information system, applied in the General Commission for Taxes, is capable of achieving its role in reducing the phenomenon of tax evasion. The existence of a set of things which in the Commission may lead to increase tax evasion by taxpa

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Publication Date
Sun Jun 02 2024
Journal Name
Journal Of Communicable Diseases
Evaluation of Susceptibility of Candida species to Six Antifungal Drugs in Iraqi Specimens
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Introduction: Candida spp. has become increasingly resistant to antifungal drugs, with elevated MIC levels causing a negative medical impact and increasing the number of patients at risk of candidiasis. According to the CDC, about 7% of Candida blood samples show reduced susceptibility to fluconazole. Monitoring the antifungal resistance profile of Candida spp. is vital, as non-Albicans species may limit treatment options. Objective: Evaluate the antifungal effectiveness against clinical Candida spp. isolates of six antifungals: amphotericin B, fluconazole, voriconazole, itraconazole, caspofungin, and 5-fluorocytosine. Methods: 100 samples were collected from various clinical samples at the National Centre of Teaching Laboratories

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Publication Date
Wed Apr 01 2015
Journal Name
Journal Of Economics And Administrative Sciences
Classification & Evaluation of Evidence of deprivation in Iraq (2009) by using Cluster analysis
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       The study aimed to reach the best rating for the views and variables in the totals characterized by qualities and characteristics common within each group and distinguish them from aggregates other for the purpose of distinguishing between Iraqi provinces which suffer from deprivation, for the purpose of identifying the status of those provinces in the early allowing interested parties and regulators to intervene to take appropriate corrective action in a timely manner. Style has been used cluster analysis Cluster analysis to reach the best rating to those totals from the provinces that suffer from problems, where the provinces were classified, based on the variables (Edu

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Publication Date
Sat Jul 01 2023
Journal Name
International Journal Of Current Medical And Applied Science
Evaluation of Postgraduate Clinical Educational Environment in The Context of Iraqi Medical Education.
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Background: A carefully planned clinical medical education is critical for the provision of supportive clinical educational environment. The latter will ensure effective teaching, active learning and good attitudes and performance at the bedside. The aim of this study was to evaluate clinical learning environment at AL-Diwaniyah Teaching Hospital. Materials and Methods: A descripitive cross-sectional study involved resident doctors from Internal Medicine and Surgery departments who had six months or more residency training in the respective departments. Data were collected using the Postgraduate Hospital Educational Environment Measure. Data where analyzed using the Statistical Package for Social Sciences version 21.0 and presented us

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Publication Date
Thu Jun 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation Of Stainless Steel Intermaxillary Fixation Screws In Treatment Of Favorable Mandibular Fractures
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Background: Numerous methods have been described for achievement of Intermaxillary fixation in the treatment of fractures of facial skeleton. Conventional methods like Erich arch bars and eyelet wires are currently the most common methods for achieving intermaxillary fixation (IMF), however, they have their own disadvantages. Since 1989, IMF using intraoral self-tapping IMF screws has been introduced for treatment of mandibular fractures. The aim of this study was to evaluate the efficacy, advantages, disadvantages and potential complications associated with using of self-tapping IMF screws in the treatment of mandibular fractures. Material and Methods: Twenty patients with favorable mandibular fractures, attended to Oral and Maxillofacial

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Publication Date
Fri Dec 15 2023
Journal Name
Bionatura
Evaluation of the quality of potable water in Al-Rusafa side, Baghdad, Iraq
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Safe drinking water is essential for the present and future generations' health. This study aims to assess drinking water quality in Baghdad's Al-Rusafa neighborhood. Water samples were taken from 32 neighborhoods on this side. The quality of the examined potable water samples differed depending on the water source. This investigation's pH, chlorine, EC, TDS, TSS, Cd, and Pb levels were below acceptable ranges. TDS levels in Al-Mada'in are more significant than acceptable (>600ppm) water levels. Bacteria have polluted six communities (Shigella, Salmonella, Escherichia coli, and Klebsiella). Bacterial quality of drinking water and gram-negative bacteria resistant to chlorine in Baghdad's municipal water supply. Regarding pH, the w

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Publication Date
Tue Sep 01 2020
Journal Name
Journal Of Engineering
Performance Evaluation of Pump Station of Main Outfall Drain in AL Nassiriyah City
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The Main Outfall drain pumping station in Nassiriyah is an important part in operation  system of the Main Outfall Drain (MOD) where it reduces the water levels in the U/S area of its and converted through Syphon freely under the Euphrates, its consists of several parts: U/S Basin, Station Building which contains 12 pumps, and Head Basin with Syphon, This station suffers from high levels especially in D/S area due to the current situation which is represented by establishing of dyke with pipes on MOD which located at 24 km from D/S of pumping station and Al-Khamisiyah Canal which located at 2.3 km from the U/S of dyke which feeds(Al Hammar Marsh) during drought season, several scenarios were adopted in order to expl

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