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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 Aug 31 2012
Journal Name
Al-khwarizmi Engineering Journal
Design a Security Network System against Internet Worms
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 Active worms have posed a major security threat to the Internet, and many research efforts have focused on them. This paper is interested in internet worm that spreads via TCP, which accounts for the majority of internet traffic. It presents an approach that use a hybrid solution between two detection algorithms: behavior base detection and signature base detection to have the features of each of them. The aim of this study is to have a good solution of detecting worm and stealthy worm with the feature of the speed. This proposal was designed in distributed collaborative scheme based on the small-world network model to effectively improve the system performance.

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Publication Date
Mon Jun 05 2023
Journal Name
Journal Of Engineering
A Computerized Integrated System for Geodetic Networks Design
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This research presents a model for surveying networks configuration which is designed and called a Computerized Integrated System for Triangulation Network Modeling (CISTNM). It focuses on the strength of figure as a concept then on estimating the relative error (RE) for the computed side (base line) triangulation element. The CISTNM can compute the maximum elevations of the highest
obstacles of the line of sight, the observational signal tower height, the contribution of each triangulation station with their intervisibility test and analysis. The model is characterized by the flexibility to select either a single figure or a combined figures network option. Each option includes three other implicit options such as: triangles, quadri

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Publication Date
Tue Apr 01 2014
Journal Name
Journal Of Economics And Administrative Sciences
Design Consolidate Cost Accounting System For Economic Entities
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      The Costing Accounting is one the analytic tools which plays important role by support the management in planning&  control and decisions-making ,as it became attendant necessity to establish any project whether industrial ,commercial ,service or agriculture ..etc.

     The consolidated accounting system has committed the companies to have their active costing system in which the management can obtain their own data, but we found most of the economic units face problems of applying the costing system because of reasons related to the system design itself or might be related to the requirements of the application success.   

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Publication Date
Tue Mar 12 2019
Journal Name
Al-khwarizmi Engineering Journal
Die Design of Flexible Multi-Point Forming Process
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Multi-point forming (MPF) is an advanced flexible manufacture technology, and the technology results from the idea that the whole die is separated into small punches that can be adjusted height. This idea is applied to the traditional rigid blank-holder, so flexible blank-holder (FBH) idea can be obtained. In this work, the performance of a multi-point die is investigated with pins in square matrix and suitable blank holder. Each pin in the punch holder can be a significant moved according to the die high and at different load that applied with spring with respect to spring stiffness. The results shows the reduction in setting time with respect to traditional single point incremental forming process that lead to (90%). and also show duri

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Publication Date
Thu Jan 01 2015
Journal Name
Journal Of Engineering
GNSS Baseline Configuration Based on First Order Design
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The quality of Global Navigation Satellite Systems (GNSS) networks are considerably influenced by the configuration of the observed baselines. Where, this study aims to find an optimal configuration for GNSS baselines in terms of the number and distribution  of baselines to improve the quality criteria of the GNSS networks. First order design problem (FOD) was applied in this research to optimize GNSS network baselines configuration, and based on sequential adjustment method to solve its objective functions.

FOD for optimum precision (FOD-p) was the proposed model which based on the design criteria of A-optimality and E-optimality. These design criteria were selected as objective functions of precision, whic

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Shield Calculation Design for gamma-ray sterilzer plant
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The present calculation covers the building shield during irradiation process and under water storage of three milion curries Cobalt-60 radiation source the calculation results in design requirement of 8m depth of water in the source stoeage pool

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Publication Date
Mon Jan 01 2024
Journal Name
Journal Of Engineering
Improvement Marshall Properties of Hot Mix Asphalt Concrete Using Polyphosphoric Acid
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Modified asphalt is considered one of the alternatives to address the problems of deficiencies in traditional asphalt concrete, as modified asphalt addresses many of the issues that appear on the pavement layers in asphalt concrete, resulting from heavy traffic and vehicles loaded with loads that exceed the design loads and the large fluctuations in the daily and seasonal temperatures of asphalt concrete. The current study examined the role of polyphosphoric acid (PPA) as a modified material for virgin asphalt when it was added in different proportions (1%, 2%, 3%, 4%) of the asphalt weight. The experimental program includes the volumetric characteristics associated with the Marshall test, the physical properties, and th

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Publication Date
Sat Jun 30 2001
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Extraction of Iron from Al-Hussainyat Iron Ore using Acid Leaching
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Publication Date
Tue Jan 01 2019
Journal Name
Indian Journal Of Public Health Research & Development
Citric Acid Production Using Wheat Bran by <i>Aspergillus niger</i>
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This study aimed to obtain a local isolation of Aspergillus niger and then studied its ability to produce citric acid from raw materials available locally using solid state fermentation. Six local isolates were collected from different sources including some samples of the damaged fruits such as grapefruit, oranges and sindi. Wheat bran was used as a raw material or as culture medium for the production of citric acid from the collected isolates. The conditions for citric acid production were determined by humidity percentage of 1: 1 (water: culture medium), temperature of 28 C, pH 4 and inoculum dose with 5× 106 spore/ml and for 3 days of incubation. The orange was the best model for citric acid production with a concentration of 12.8 mg/m

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Publication Date
Sun Sep 01 2019
Journal Name
Civil Engineering Journal
Effect of PolyPhosphoric Acid on Rutting Resistance of Asphalt Concrete Mixture
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The action of high repeated trucks load associated with dramatically elevated ambient temperatures leads to the most harmful distress in asphalt pavements occurred in Iraq known as rutting. Essentially, it is produced from the accumulation of irrecoverable strains, which mainly occurred in the asphalt layers. That visually demonstrated as a longitudinal depression in the wheel paths as well as small upheavals to the sides. Poly Phosphoric Acid (PPA) has been used as a means of producing modified asphalt binders and the interest to use it has increased in recent years. The PPA provides modified asphalt binder, which is relatively cheaply produced compared to polymer-modified asphalt. In this paper, PPA was used by three-percentages 1

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