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New Niflumic Acid Derivatives as EGFR Inhibitors: Design, Synthesis, In silico Studies, and Anti-proliferative Assessment
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Background:

1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.

Objectives:

To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.

Methods:

The designed compounds were synthesized using conventional organic synthesis methods. The antitumor activities of the new NF derivatives against HepG2 hepatocellular carcinoma and A549 non-small cell lung cancer cell lines were assessed in vitro via MTT assay, flow cytometry, RT-PCR, as well as via molecular docking studies.

Results:

The cytotoxicity results indicated that the newly synthesized NF derivatives were cytotoxic against the two cancer cell lines, with compound 6 being the most cytotoxic, achieving the lowest IC50 concentration. Furthermore, compound 6 targeted EGFR tyrosine kinase leading to cell cycle arrest at the G2/M cell cycle phase and induction of apoptosis. The in vitro biological investigation results matched those of the molecular docking analysis. In conclusion, the new NF derivatives, specifically compound 6, exhibited favorable pharmacokinetic features and are promising EGFR tyrosine kinase inhibitors.

Conclusion:

A series of niflumic acid derivatives (3, 4A-E, 5, and 6) were successfully created, and FT-IR, 1H, 13CNMR, and HRMS were used to confirm their chemical structures. According to molecular docking studies, compounds 3, 5, and 6 have the highest docking scores (ΔG), and most tested compounds have a good pharmacokinetic profile. Results of compound 6 in vitro antitumor activities showed that it is a promising EGFR tyrosine kinase inhibitor.

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Publication Date
Fri Jun 30 2023
Journal Name
Journal Of The College Of Education For Women
The Degree of Using Augmented Reality Technology among students of the Optimum Invesment Project fot Teaching Personnel Program and the difficulties they face at Al-Shaqra University
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Augmented reality technology is a modern technique used in all fields, including: medicine, engineering and education, and has received attention from officials in the educational process at present; The focus of this research is on the degree of use of augmented reality among field experience students in the project's optimal investment program for teaching staff and their difficulties, applied to a sample of 75 students, through a questionnaire prepared by the researcher as a tool to determine the degree of use, as well as difficulties. The researcher addressed the subject through two main axes to determine the degree of use, as well as the difficulties preventing teachers and learners from using this technique. The results of the rese

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Publication Date
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
A Theoretical Investigation of Chemical Bonding of a Heterometallic Trinuclear Cluster Containing Iridium and Ruthenium: [(Cp*Ir) (CpRu)2 (μ3-H) (μ-H)3] by QTAIM Approach
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  Numerous integral and local electron density’s topological parameters of significant metal-metal and metal-ligand bonding interactions in a trinuclear tetrahydrido cluster [(Cp* Ir) (Cp Ru)2 (μ3-H) (μ-H)3]1 (Cp = η5 -C5Me5), (Cp* = η5 -C5Me4Et) were calculated and interpreted by using the quantum theory of atoms in molecules (QTAIM). The properties of bond critical points such as the delocalization indices δ (A, B), the electron density ρ(r), the local kinetic energy density G(r), the Laplacian of the electron density ∇2ρ(r), the local energy density

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Publication Date
Wed Aug 17 2022
Journal Name
Al–bahith Al–a'alami
Lawyers’ Use of the Website of the Supreme Judicial Council and the Gratifications Obtained from It Drawn Research Submitted for the Study of the Higher Professional Diploma
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The field study of this paper focused on the motives for lawyers to use the website
of the Supreme Judicial Council, and the gratifications achieved as a result of its use.
This study sought to achieve a number of goals, including:
1. Monitoring the patterns of lawyers’ use of the website of the Supreme Judicial Council.
2. Determining the forms that lawyers use to interact on the website of the Supreme
Judicial Council.
This study is a descriptive in kind as the researcher relied on the ‘survey method’ in
its study of the external audience (lawyers) using the questionnaire and scale toolThe questionnaire was distributed among a deliberately chosen sample, consisting of
(160) lawyers who used the website of

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Publication Date
Wed Jan 10 2024
Journal Name
Nanotechnology
Improving the targeted delivery of curcumin to esophageal cancer cells via a novel formulation of biodegradable lecithin/chitosan nanoparticles with downregulated miR-20a and miR-21 expression
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Abstract<p>Nanoencapsulation, employing safe materials, holds substantial promise for enhancing bioactive compounds’ delivery, stability, and bioactivity. In this study, we present an innovative and safe methodology for augmenting the incorporation of the anticancer agent, curcumin, thereby inducing apoptosis by downregulating miR20a and miR21 expression. Our established methodology introduces three pivotal elements that, to our knowledge, have not undergone formal validation: (1) Novel formulation: We introduce a unique formula for curcumin incorporation. (2) Biocompatibility and biodegradability: our formulation exclusively consists of biocompatible and biodegradable constituents, ensuring t</p> ... Show More
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Publication Date
Wed Aug 31 2022
Journal Name
Al-kindy College Medical Journal
Antimicrobial Activity of Lepidium Sativum against Multi drug resistant and sensitive Pseudomonas aeruginosa from clinical isolates, Khartoum State, Sudan: Lepidium Sativum against Clinical isolates of Pseudomonas aeruginosa
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Background: L. sativum, are traditionally used for the treatment of various diseases and thought to have medicinal value. Isolates from many part of the world is now multidrug resistant. Therefore, there is an urgent need to look for and test an alternative herbal drug.

Objective: The present study aimed to evaluate the antibacterial activity of L. Sativum seed extract against multi drug resistant (MDR) and sensitive Pseudomonas aeruginosa clinical isolates.

Subjects and Methods: An ethanolic and aqueous stock extracts were prepared from L.  sativum seed plant then serial dilutions were prepared and the obtained concentrations (50, 25, 12.5 and 6.2 mg/ml) were tested against 30 multidrug-resistan

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Publication Date
Mon Jun 01 2015
Journal Name
Journal Of Economics And Administrative Sciences
Theories of the structure of modern finance : practical application of pecking order theory and the life cycle of the company/analytical research of asmple of foreign companies
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 Is the subject of the financial structure of the most important topics for which she received the interests of scientific research in the field of financial management , as it emerged several theories about choosing a financial structure appropriate for the facility and behavior change funding them , and in spite of that there is no agreement on a specific theory answer various questions in this regard , and a special issue of the financial structure optimization.

The objective of the research was to identify the most important theories of the structure of modern financial theory has been to focus on the capture of financial firms in two different stages of their life cycle , so-called growth and ma

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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
Measuring the speed of response of the exported quantity of crude oil to the increase in its prices using the model Impulse Response Functions (IRF) (Iraq case study) for the period (1978-2017)
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Abstract

     Oil is considered a commodity and is still an important and prominent role in drawing and shaping the Iraqi economic scene. The revenues generated from the export of oil are considered the main source of the general budget in cash flows.  

     Since the revenues consist of quantity and price and the latter is an external factor which is difficult to predict, The effect of any commodity on its price, which is proven in the theory of micro-economic, but it is observed through the research that the response is slow, which means not to take advantage of the rise in prices, by increasing the quantity exported, the result of several facto

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Publication Date
Tue May 16 2023
Journal Name
Political Sciences Journal
The Impact of Putinism on the Russian-Ukrainian Conflict: an analysis of the contents of the speeches of Russian President Vladimir Putin on the causes of the Russian war on Ukraine in 2022
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this research seeks to shed light on the study of the impact of Putinism on the Russian-Ukrainian war that broke out in early 2022, by studying the contents of the speeches of Russian President Vladimir Putin before the start of the war. This research uses the structural approach in analyzing the components of the Russian political regime. The research tools used in this research include case studies, content analysis of Russian speeches, and personal meetings of researchers and specialists in Russian affairs. It sums up a number of important conclusions, most notably are : 1) Putinism is a totalitarian regime that includes the political doctrine during the era of Russian President Vladimir Putin. 2) Duginism represents the totality of t

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Publication Date
Mon Oct 05 2026
Journal Name
Al–bahith Al–a'alami
Graduate Media Students’ Satisfaction Level in Their Program of Study:  The level of Satisfaction about the Study Programs of the masters of Media students / Case Study of Media faculties’ students at “Yarmouk University,
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The current study is considered a field study to measure the level of satisfaction of the academic programs of Media Masters students. That was accomplished through surveying the attitudes of the students who are enrolled in the faculties of media at the following universities: (Petra University, The Middle East University (MEU), and Al-Yarmouk University). Those students were enrolled in the master’s program within the formal educational system during the second semester of the academic year (2015 – 2016). This survey aims to identify the services, facilities and academic programs provided by the concerned faculties. It, also, aims to identify the public relations, administrative, educational and services aspects of those faculties.

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Publication Date
Sun Jun 22 2025
Journal Name
اكليل للدراسات الانسانية
Topic review article Britain and Iraq's book The Economic Status of Iraq during the era of the British administration 1914-1921 by Dr. Hussein Ali Falih Al-Khazraji
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: Summary Iraq suffered under the British administration during the First World War and its entry into an occupation of economic backwardness, and this economic backwardness was linked to the phenomenon of linking Iraq economically to the capitalist world by keeping it as a source of raw materials and a market for capitalist goods, and that the occupation authorities controlled Iraq's economic goods and wealth and mocked them to serve its interests and achieve their political and economic goals that it drew before the war.

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