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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
Mon Mar 25 2019
Journal Name
Al-academy
The Effectiveness of Implication in New Formulations of the Contemporary Industrial Product: زياد حاتم حربي
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  The current research aims at transforming the concept of implication from the rhetoric into the industrial design in order to have a new term (the design implication) in which the industrial designer takes all or part of another's design to imply his design in it and acknowledge that, and if he did not do so, it would be (design theft) parallel to the literary plagiarism.
In order to show the potentials of the industrial design in the production of new formulations of the industrial products forms, as the design is the carrier of language that addresses the recipients, it is possible to use the implication as a the tool of literature in the design and as a design strategy as it is one of the concepts that takes its course in e

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Publication Date
Sun Sep 22 2019
Journal Name
Baghdad Science Journal
New record of three species of Leeches (Annelida:Hirudinea) in Al-Hindyia River / Babil Province / Iraq
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In this study, a total of 209 individuals of leeches were collected from Al-Hindyia River / Babil Province. 116 individuals were identified as Erpobdella octaculata (Linnaeus, 1758), 50 individuals as Erpobdella punctata (Leidy,1870) and  43 individuals as Hemiclepsis marginata (Müller, 1774).  Four samples were collected monthly during a period from February to June 2018. Some physical and chemical water properties were also examined, including air and water temperature, potential of hydrogen pH, Electrical Conductivity EC, Total Dissolved Solid TDS, Dissolved Oxygen DO, and the Biological Oxygen Demand BOD₅.  Air and water temperature were r

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Publication Date
Mon Dec 24 2018
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
A NEW RECORD OF COELASTRELLA TERRESTRIS (REISIGL) HEGEWALD & N. HANAGATA, 2002 (SPHAEROPLEALES, SCENEDESMACEAE) IN IRAQ
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    This study identified the genus Coelastrella Chodat, 1922 which was isolated from a sediment sample taken from the Tigris river in Baghdad Governorate, Iraq. The alga was isolated and cultured in modified Chu 10 media and the morphological features of the isolated algae were observed in light microscopy (LM); it showed some characteristic features of this genus, such as its ellipsoidal or lemon- shaped cells, a visible pyrenoid and the chloroplast parietal. To ensure correct identification of the isolated alga, a molecular analysis using 18S rRNA gene and DNA sequencing revealed a match with C. terrestris (Reisigl) Hedewald & N. Hanagata 2002. This species is a new record in Iraq

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Publication Date
Mon Apr 28 2025
Journal Name
Chemical Papers
New chemiluminometric method for the determination of azithromycin in a continuous flow injection analysis system
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A novel analytical method is developed for the determination of azithromycin. The method utilizes continuous flow injection analysis to enhance the chemiluminescence system of luminol, H2O2, and Cr(III). The method demonstrated a linear dynamic range of 0.001–100 mmol L-1 with a high correlation coefficient (r) of 0.9978, and 0.001–150 mmol L-1 with a correlation coefficient (r) of 0.9769 for the chemiluminescence emission versus azithromycin concentration. The limit of detection (L.O.D.) of the method was found to be 18.725 ng.50 µL−1 based on the stepwise dilution method for the lowest concentration within the linear dynamic range of the calibration graph. The relative standard deviation (R.S.D. %) for n = 6 was less than 1.2%

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Publication Date
Fri Jan 01 2016
Journal Name
Computational Intelligence And Neuroscience
A New Artificial Neural Network Approach in Solving Inverse Kinematics of Robotic Arm (Denso VP6242)
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This paper presents a novel inverse kinematics solution for robotic arm based on artificial neural network (ANN) architecture. The motion of robotic arm is controlled by the kinematics of ANN. A new artificial neural network approach for inverse kinematics is proposed. The novelty of the proposed ANN is the inclusion of the feedback of current joint angles configuration of robotic arm as well as the desired position and orientation in the input pattern of neural network, while the traditional ANN has only the desired position and orientation of the end effector in the input pattern of neural network. In this paper, a six DOF Denso robotic arm with a gripper is controlled by ANN. The comprehensive experimental results proved the appl

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Publication Date
Thu Jul 01 2021
Journal Name
Solar Energy
A new approach for employing multiple PCMs in the passive thermal management of photovoltaic modules
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Publication Date
Tue Jun 30 2015
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Preparation and Characterization of Y2O3, Sio2 Doped By Eu2O3 as Luminescent Ink
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   This article includes the preparation of luminescence materials from rare earth (Eu ) ion doping Yttrium Oxide (Y2O3) 70% and SiO2 25% and study the characteristics of phosphors for ultraviolet to visible conversion. The phosphor materials have been synthesized by two steps: Preparing the powder by solid state method using Y2O3, SiO2 and Eu2O3 with doping materials concentration (70%, 25% and 5%) respectively and different calcination temperature (1000, 1200 and 1400 oC).

   The second step is to prepare the colloid solution by dispersing the produced powder in a polyvinyl alcohol solution (4%) .

Powde

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of The College Of Languages (jcl)
Individualism and the Symbolic Language of Imagination (Pablo Neruda as an Example)
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Pablo Neruda's artistic distinctiveness can be considered in two ideas or attitudes of romanticism. First, the imagination, which is the result of conduct and spirituality, and second, the individualism, which is a collection of mysterious mysteries from the texts of individuality based on philosophical sonnets. His collection of poems points out the ethereality and indescribability of life, employing the reality of life at the level of human perception in a symbolic language. In other words, Pablo Neruda recreates the meanings in poetry through the three ideas of reduction, interpretation, and analysis. "What is the essential connection between individualism and the symbolic language of Pablo Neruda's imagination and What are the reason

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Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents
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The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Piroxicam as Self-Nano Emulsifying Drug Delivery System
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Piroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin

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