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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 Jan 01 2021
Journal Name
Journal Of Economics And Administrative Sciences
The influence of organizational culture on the organizational performance of educational institutions (University of Technology as a model)
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The organizational culture is an effective control mechanism that dictates the behavior of employees and according to their intellectual and social orientations, so it is considered a more powerful way to control employee orientations and determine their management according to organizational rules and regulations, as it was one of the most important factors determining the performance of organizations, while organizational performance is a measure of what the organization has achieved from the objectives of the scheme To ensure that it faces various changes and remains within the global competition, and to reach that it was necessary to identify the most prominent and most important research problems in knowing the extent of com

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Publication Date
Fri Mar 01 2024
Journal Name
Nano Biomedicine And Engineering
Silver Nanoparticles Synthesized by Cold Plasma as an Antibiofilm Agent against <i>Staphylococcus epidermidis</i> Isolated from Acne
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silver nanoparticle which synthesized by.

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Publication Date
Wed Mar 04 2026
Journal Name
Al–bahith Al–a'alami
MOTIVES FOR STUDENTS TO BE EXPOSED TO EDUCATIONAL PROGRAMS ON TV CHANNELS (Iraqi educational channels as a model)
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The educational function of television is one of the basic functions in light of the technical development that included the specialized satellite channels in all its fields, including the educational field, as its role became parallel to the role of educational institutions. These studies are among the descriptive studies in terms of the type of study methodology that describes the phenomenon, interprets its and extract the results and relationships between the variables. The study sample was multistage (random and intentional) included the students of the sixth academic and literary preparatory stage in the city of Baghdad.
The study problem was summarized by the following main question:
( What are the motives for the exposure of

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Publication Date
Mon Sep 30 2024
Journal Name
Iraqi Journal Of Science
Use of Scalp Hair as a Biomarker to Determine Airborne Heavy Metal Concentrations for the Academic Laboratory Employees
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Academic chemical laboratories (ACL) are considered public places  the employees come in contact with a variety of pollutants. The aim of the current study was to detect heavy metals levels in the indoor air of ACL in two universities in Baghdad city and assess their levels in the academic employees’ scalp hair as biomarkers. Air samples inside ACL were collected to detect Fe, Cd, Zn, Pb and Cu. Scalp hair samples were collected from 40 adult chemical laboratory employees aged 30-60 years, who worked 5 days/week for 6 hours a day. Personal information relating to employees such as age, duration of exposure, smoking habit and sex, was collected as a questionnaire. The results of this study concluded that academic laboratory employ

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Publication Date
Wed Mar 04 2026
Journal Name
Al–bahith Al–a'alami
The Reliance of the Public of Baghdad on News Broadcasts on Satellite Channels as a Source of Information
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The importance of news broadcasts in society has increased after the domination of television over the mass media, especially after emerging the satellite channels, and spreading the satellite dishes among the public at large.

As well as the great role played by the modern technology in the transmission of news and events happening at once. Such role has contributed, significantly, in changing the concept and values ​​of the news. The live broadcast of the events filmed is the news itself.

In the midst of the great transformations and circumstances that Iraq went through after 2003, which witnessed political and security instability, and the large increase in the number of media, especially satellite channels, in Iraq

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Publication Date
Wed Jul 01 2015
Journal Name
Al–bahith Al–a'alami
The Position of the Oil Press about the World Oil Industry / OAPEC Bulletin 2011-2012 as a Model
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This research deals with the attitude of oil press towards oil industry in the world and the extent of their concerns with the stages of oil industry relating to the abundance of oil and natural gas, as it is an international strategic and complementary industry. The researcher uses the survey method for content analysis of the initial article and the press news for two: years (2011-2012). The results if the study are as follows
1- Oil press is concerned with developing and the stages of the Arabic oil industry in the interest of OAPEC in the first place.
2- It is concerned with exploring, extracting, and marketing oil in the first place, then with refining operations in refineries and petrochemical plants in the second place, an

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Publication Date
Wed Oct 04 2023
Journal Name
Environmental Progress &amp; Sustainable Energy
Removal of <scp>E133</scp> brilliant blue dye from artificial wastewater by electrocoagulation using cans waste as electrodes
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Abstract<p>Solid‐waste management, particularly of aluminum (Al), is a challenge that is being confronted around the world. Therefore, it is valuable to explore methods that can minimize the exploitation of natural assets, such as recycling. In this study, using hazardous Al waste as the main electrodes in the electrocoagulation (EC) process for dye removal from wastewater was discussed. The EC process is considered to be one of the most efficient, promising, and cost‐effective ways of handling various toxic effluents. The effect of current density (10, 20, and 30 mA/cm<sup>2</sup>), electrolyte concentration (1 and 2 g/L), and initial concentration of Brilliant Blue dye (15 and 30 mg/L) on </p> ... Show More
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Publication Date
Wed Dec 22 2021
Journal Name
Antibiotics
Classic vs. Novel Antibacterial Approaches for Eradicating Dental Biofilm as Adjunct to Periodontal Debridement: An Evidence-Based Overview
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Periodontitis is a multifactorial chronic inflammatory disease that affects tooth-supporting soft/hard tissues of the dentition. The dental plaque biofilm is considered as a primary etiological factor in susceptible patients; however, other factors contribute to progression, such as diabetes and smoking. Current management utilizes mechanical biofilm removal as the gold standard of treatment. Antibacterial agents might be indicated in certain conditions as an adjunct to this mechanical approach. However, in view of the growing concern about bacterial resistance, alternative approaches have been investigated. Currently, a range of antimicrobial agents and protocols have been used in clinical management, but these remain largely non-v

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Publication Date
Thu Sep 01 2016
Journal Name
Journal Of Engineering
Effect of Using Porcelanite as Partial Replacement of Fine Aggregate on Roller Compacted Concrete with Different Curing Methods
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Roller-Compacted Concrete is a no-slump concrete, with no reinforcing steel, no forms, no finishing and wet enough to support compaction by vibratory rollers. Due to the effect of curing on properties and durability of concrete, the main purpose of this research is to study the effect of various curing methods (air curing, 7 days water curing, and permanent water curing) and porcelanite (local material used as an Internal Curing agent) with different replacement percentages of fine aggregate (volumetric replacement) on some properties of Roller-Compacted Concrete and to explore the possibility of introducing practical Roller-Compacted Concrete for road pavement with minimum requirement of curing. Specimens were sawed fro

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Publication Date
Mon Aug 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of Tetradentate Complexes Type N2O2 From the Reaction of 2-Hydroxy -1, 2-Diphynel-Ethanone Oxime [H2L] With Mn II, Fe II, Co II, Ni II, Cu II and Hg II Ions
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Tetradentate complexes type [M (HL) 2] were prepared from the reaction of 2-hydroxy -1, 2-diphynel-ethanone oxime [H2L] and KOH with ( Mn II, Fe II, Co II, Ni II , Cu II and Hg II ), in methanol with (2:1) metal: ligand ratio. The general formula for Cu II and Mn II complexes are [M (HL) 2 Cl.H2O] K, for Co II [Co (HL) 2. H2O] and [M (HL) 2] for the rest of complexes. All compounds were characterised by spectroscopic methods, I.R, U.V-Vis, H.P.L.C, atomic absorption and conductivity measurements chloride content. From the data of these measurements, the proposed molecular structures for Fe II and Hg II complexes are tetrahedrals, while Mn II and Cu II complexes are octahedrals, Ni II complex adopting square planar structure and the complex

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