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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
Wed Feb 04 2026
Journal Name
Journal Of Physical Education
Standard Criteria for Some Special Abilities as Indicator for Selecting Iraqi Club's Weightlifters Aged 14 – 16 years Old
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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Clinical And Experimental Dentistry
Eradication of mature biofilm from the isthmus region using Er, Cr: YSGG Laser as an activator of 2% chlorhexidine gluconate
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Publication Date
Sat Jul 19 2025
Journal Name
Journal Of Pharmacology And Pharmacotherapeutics
Pharmaceutical Frontliners: Community Pharmacists’ Contribution to Managing Medication Needs During a Health Crisis— The COVID-19 Era as an Example
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Community pharmacists faced more complex challenges in meeting patients’ medication needs during the pandemic than previously reported in the literature. Objectives To explore the perception and abilities of community pharmacists in managing patients’ needs in terms of medication dispensing during the pandemic, and to examine its effect on improving the patients’ situations. Materials and Methods A cross-sectional study design, validated by 30 experts, was conducted using an electronic survey (Google Form) to assess the effect of the dispensing practice of Iraqi community pharmacists on the patient’s clinical outcomes during the pandemic. The survey was distributed on professional pharmacist’s social media platforms from December

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Publication Date
Tue Mar 12 2024
Journal Name
مداد الآداب
“As if sky was blue”: An Eco-Marxist Reading of Caryl Churchill’s Play Not Not Not Not Not Enough Oxygen
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 Humanity is confronted with a growing array of environmental challenges that demand immediate attention and cannot be disregarded. One of the issues the world faces is air pollution, which presents a significant risk to both the environment and human well-being. The capitalist system has a great impact on the exacerbation of air pollution and environmental deterioration. This impact is reflected in Caryl Churchill’s post-apocalyptic play Not Not Not Not Not Enough Oxygen (1971). The play presents a futuristic scenario in which humanity faces grave consequences due to the polluting practices of capitalism and the unsustainable exploitation of natural resources. It depicts a future in which environmental degradation drives people

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Publication Date
Tue Jan 31 2017
Journal Name
Journal Of Engineering
Determine an Equation to Calculate the Annual Maintenance Cost for Public Hospitals (Al Sader City Hospital as a Case Study)
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Maintenance of  hospital buildings and its management are regarded as an important subject which needs attention because hospital buildings are service institutions which are very important to a society, requiring the search for the best procedure to develop maintenance in hospitals. The research is aimed to determine an equation to estimate the annual maintenance cost for public hospital. To achieve this aim, Al-Sader City Hospital maintenance system in Al-Najaf province has been studied with its main elements through survey of data, records and reports relating to maintenance during the years of the study 2008-2014 and to identify the strengths, weaknesses, opportunities and threat points in the current system through Swat analysi

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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
Degradation of Brilliant Green by Using a bentonite Clay- Based Fe Nano Composite Film as a Heterogeneous Photo- Fenton Catalyst.
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This paper aims to study the chemical degradation of Brilliant Green in water via photo-Fenton (H2O2/Fe2+/UV) and Fenton (H2O2/Fe2+) reaction. Fe- B nano particles are applied as incrustation in the inner wall surface of reactor. The data form X- Ray diffraction (XRD) analysis that Fe- B nanocomposite catalyst consist mainly of SiO2 (quartz) and Fe2O3 (hematite) crystallites. B.G dye degradation is estimated to discover the catalytic action of Fe- B synthesized surface in the presence of UVC light and hydrogen peroxide. B.G dye solution with 10 ppm primary concentration is reduced by 99.9% under the later parameter 2ml H2O2, pH= 7, temperature =25°C within 10 min. It is clear that pH of the solution affects the photo- catalytic degradation

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Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
The efficiency of Paecilomyce farinosus as biocontrol to larve stage on second ad sixith instar larve of Trogoderma granarium (Everts)
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The present study was conducted to determine the pathogenicity of Paecilomyces farinosus as biocontrol agents against Tragoderma granarium (khapra) under laboratory conditions with three concentrations ( 2.8 x 108 , 2.8 x 106 ,2.8 x104 spores/ ml). The laboratory results revealed that fungi showed it's higher pathogencity to larve stage on 2nd instar and 6th instar , although their capability differs according to the fungi concentrations this fungi caused higher mortality of 2nd larval instar 70% and 60% ,55% when it was used at concentrations 2 .8 x 106 ,2.8 x104 spores/ ml respectively. On the other hand on 6th larval instars 55% , 35% , 30% at concentrations ( 2.8 x 108 , 2.8 x 106 ,2.8 x104 spores/ ml) respectively, and the h

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Publication Date
Wed Feb 04 2026
Journal Name
Adab Al Rafidayn
Measuring the quality of office services using (LibQUAL + ®): the central library of the University of Baghdad as a model
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Libraries, information centers, and everything related to organizing and preparing information need to be periodically re-evaluated in order to stand on the level of quality, which means improving the general reality of these institutions to ensure sufficient satisfaction from beneficiaries of the services provided. This is what was worked on in this research, as one of the most important quality standards in libraries and information centers, LibQUAL+®, was applied in one of the most important and oldest central university libraries, namely the Central Library of the University of Baghdad at its two locations, Al-Jadriya and Al-Waziriya. The sample of beneficiaries to whom the questionnaire was distributed reached 75 beneficiaries distrib

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Publication Date
Wed Dec 13 2017
Journal Name
Al-khwarizmi Engineering Journal
Using Activated Carbon developed from Iraqi Date Palm Seeds as Permeable Reactive Barrier for Remediation of Groundwater Contaminated with Copper
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The possibility of using activated carbon developed from date palm seeds wastes as a permeable reactive barrier (PRB) to remove copper from polluted shallow groundwater was investigated. The activated carbon has been developed from date palm seeds by dehydrating methods using concentrated sulfuric acid. Batch tests were performed to characterize the equilibrium sorption properties of new activated carbon in copper-containing aqueous solutions, while the sandy soil (aquifer) was assumed to be inert. Under the studied conditions, the Langmuir isotherm model gives a better fit for the sorption data of copper by activated carbon than other models. At a pilot scale, One-dimensional column experiments were performed, and an integrated model ba

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Publication Date
Wed Jan 13 2021
Journal Name
Egyptian Journal Of Chemistry
Development of a nanostructured double-layer coated tablet based on polyethylene glycol/gelatin as a platform for hydrophobic molecules delivery
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The aim of the current study was to develop a nanostructured double-layer for hydrophobic molecules delivery system. The developed double-layer consisted of polyethylene glycol-based polymeric (PEG) followed by gelatin sub coating of the core hydrophobic molecules containing sodium citrate. The polymeric composition ratio of PEG and the amount of the sub coating gelatin were optimized using the two-level fractional method. The nanoparticles were characterized using AFM and FT-IR techniques. The size of these nano capsules was in the range of 39-76 nm depending on drug loading concentration. The drug was effectively loaded into PEG-Gelatin nanoparticles (≈47%). The hydrophobic molecules-release characteristics in terms of controlled-releas

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