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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
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Serum ceruloplasmin ,copper and iron levels as a risk factors for coronary heart diseases(CHD)
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Ceruloplasmin (Cp) is one of the acute phase protein, in this review ,we studied the level of ceruloplasmin with copper (Cu) and iron in 90 patients with coronary heart diseas ( those patients are divided into three groups, whom are stable angina , unstable angina and myocardial infarction compared with 30 healthy volunteers) and the roles of them as diagnostic and prognostic tools.The diagnosis was attend by a clinical examination carried out by the consult medical staff in Ibn AL-Nafis hospital. The result: ceruloplasmin recorded a significantly(p<0.05)higher level in all patient groups compared with the control, so this result supports the hypothesis that a high serum ceruloplasmin level is a risk factor for coronary heart di

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Publication Date
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
The Mental Disorder of mothers as a Mediating Variable Between Marital adjustment and Kindergarteners Development
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This current study aimed to explore the mediation effects of mother's mental health symptoms between marital adjustment and child development aspects. (666) participants of mothers and their children were the sample of the study. The researchers used the marital adjustment scale prepared by Manson, Morse, Lerner, Arthur, as well as, a package of tests for some aspects of growth Kindergarten children prepared by Kenawi and Mohamed (1999). In addition, theyemployed a list of modified symptoms (Symptom Checklist-90- Revised (SCL) -90-, prepared by Derogatis, Lipman and Lipogun & Cov (1976), The results of the current study showed there is a statistically significant relationship between marital adjustment and the symptoms of mental diso

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Publication Date
Sun Mar 04 2012
Journal Name
Baghdad Science Journal
Phase transformation study of Iraqi Bentonite with Al2O3 and MgO as additions at high temperatures
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Iraqi bentonite is used as main material for preparing ceramic samples with the additions of alumina and magnesia. X-ray diffractions analyses were carried out for the raw material at room temperature. The sequence of mineral phase's transformations of the bentonite for temperatures 1000 ,1100 ,1200 and 1250 ºC reflects that it finally transformed in to mullite 39.18% and cristobalite 62.82%. Samples of different weight constituent were prepared. The effect of its constitutional change reveals through its heat treatments at 1000,1100,1200,1250and 1300ºC .The samples of additions less than 15% of alumina and magnesia could not stand up to 1300ºC while the samples of addition more than 15% are stable .That is shown by analy

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Publication Date
Thu May 14 2020
Journal Name
Journal Of Planner And Development
Visual Pollution and its Impact on the Aesthetics: The Town of Eizariya as a Model
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This study seeks to shed light on the aspects of visual pollution and its impact on the aesthetics of the town of Al-Eizariya known to suffer from the phenomenon. In order to identify the real causes of the problem which develops in various forms and patterns, threatening not only the aesthetic appearance of the towns, but also causes the emergence of new problems and phenomena that will have negative repercussions on the population. The researcher uses the analytical descriptive method to analyze the phenomenon of visual pollution in terms of reality, development, manifestations and spread and uses photos which document the visual pollution and its impact on the aesthetics of the known. The study concluded the existence of a strong rela

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Publication Date
Tue Jun 01 2021
Journal Name
Baghdad Science Journal
Mesoporous Silica Nanoparticles as a System for Ciprofloxacin Drug Delivery; Kinetic of Adsorption and Releasing
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Mesoporous silica (MPS) nanoparticle was prepared as carriers for drug delivery systems by sol–gel method from sodium silicate as inexpensive precursor of silica and Cocamidopropyl betaine (CABP) as template. The silica particles were characterized by SEM, TEM, AFM, XRD, and N2adsorption–desorption isotherms. The results show that the MPS particle in the nanorange (40-80 nm ) with average diameter equal to 62.15 nm has  rods particle morphology, specific surface area is 1096.122 m2/g, pore volume 0.900 cm3/g, with average pore diameter 2.902 nm, which can serve as efficient carriers for drugs. The adsorption kinetic of Ciprofloxacin (CIP) drug was studied and the data were analyzed and found to match well with

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Publication Date
Sat Apr 01 2023
Journal Name
Journal Of Engineering
Estimation of Water and Energy Saving by Rainwater Harvesting: Sulaimani City as a Case Study
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Rainwater harvesting could be a possible solution to decrease the consequences of water scarcity and energy deficiency in Iraq and the Kurdistan Region of Iraq (KRI). This study aims to calculate the water and energy (electricity) saved by rainwater harvesting for rooftops and green areas in Sulaimani city, KR, Iraq. Various data were acquired from different formal entities in Sulaimani city. Moreover, Google Earth and ArcMap 10.4 software were used for digitizing and calculating the total rooftop and green areas. The results showed that for the used runoff coefficients (0.8 and 0.95), the harvested rainwater volumes were 2901563 and 12197131 m³ during the study period (2005 – 2006) and (2019-2020). Moreover, by compa

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Publication Date
Thu Jan 10 2019
Journal Name
Journal Of The College Of Education For Women
Intellectual and Religious Characteristics Andalusion Societ Image Beni Al-Ahmar Era Poetry as a model
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The intellectual and religious characteristics were an influential presence in the same Andalusian poet, especially among the poets of Beni El-Ahmar because they are part of the heritage of poets, and that is to push them towards the glory of this heritage and to take care of it and benefit from its inclusion, inspiration and similarity.

That this inflection on the poetic heritage is justified by the poets of the sons of the Red were inclined to preserve the inherited values, especially as it was related to their poetry, especially that the Andalusian poet did not find embarrassment in the inspiration of heritage and emerged when he mentioned the homes and the ruins and the camel and the journey, although the community Andalusian

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Publication Date
Mon Jan 05 2009
Journal Name
J. Duhok Univ
The role of red pigment produced by Serratia marcescens as antibacterial and plasmid curing agent
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Publication Date
Fri Jan 01 2016
Journal Name
Arpn Journal Of Engineering And Applied Sciences
Implementation And Evaluation Of Apm 2.6 - Controlled Quadcopter With Aerial Imagery As A Case Study
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Publication Date
Sat Nov 01 2025
Journal Name
Construction And Building Materials
Polyalphaolefin as a potential modifying agent for hard asphalt cement: Physical, rheological, and chemical characterization
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Hard-grade asphalt binders like AC20-30 typically exhibit excessive stiffness, reduced penetration, and compromised workability, necessitating modification before use in paving applications. This study evaluates the efficacy of regular polyalphaolefin (PAO), a synthetic olefin-based lubricant, as a performance-enhancing modifying agent for such binders. AC20-30 was blended with PAO at dosages ranging from 2 wt.% to 10 wt.%, and the modified binders were characterized via penetration, ductility, softening point, and rotational viscosity measurements, alongside advanced rheological and chemical-morphological analyses. Incorporating PAO in AC20-30 asphalt progressively reduced the binder stiffness and enhanced its flexibility, with all modifie

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