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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 Jun 19 2023
Journal Name
Journal Of Engineering
Experimental Studies and Finite Element Modeling of Piles and Pile Groups in Dry Sand under Harmonic Excitation
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Foundations supporting reciprocating engines, radar towers, turbines, large electric motors, and generators, etc. are subject to vibrations caused by unbalanced machine forces as well as the static weight of the machine. If these vibrations are excessive, they may damage the machine or cause it not to function properly. In the case of block foundation, if changes in size and mass of the foundation do not lead to a satisfactory design, a pile foundation may be used. In this study, the dynamic response of piles and pile Groups in dry sand is investigated experimentally. The analysis involves the displacement response under harmonic excitation. In addition, a numerical modeling by using finite element method with a three-dimensional formula

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Publication Date
Sat Sep 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Petroleum Derivatives in Iraq The phenomenon of Renewable or Passing crisis
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     Iraq economy suffered, nor , still many difficulties and problems , including oil derivatives crisis that emerged in 2004 and was the most prominent features of the inability of local production to meet the needs of the increasing growth of consumption, the crisis has cast a shadow on the growth of national in general, and citizen living in particular. Therefore, the real test of crisis and challenge to the capacity of government agencies to manage the crisis and control and reduce its harmful effects, which disappear in a region or sector, even begin to appear in another, given the multiplicity and complexity of third-party solution for remedying the negative consequences of deliberate.

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Publication Date
Tue Jan 02 2018
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Multiple choice questions and essay questions in assessment of success rate in medical physiology
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Background: Assessment is an important part of the learning cascade in education. Students realize it as an influential motivator to direct and guide their learning. The method of assessment determines the way the students reach high levels of learning. It has been documented that one of factor affecting students’ choice of learning approach is the way how assessment is being performed. Many methods of assessment namely multiple choice questions, essay questions and others are mainly used to assess basic science knowledge in undergraduate education. Objectives: The aim of this study is to compare multiple choice questions (MCQ) and essay questions (EQ) (record the success and failure rate of multiple choice questions (MCQ) and essay quest

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Publication Date
Sun Sep 01 2013
Journal Name
Applied Mechanics And Materials
Artistic Techniques for Developing Creativity in Design
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The design of future will still be the most confusing and puzzling issue and misgivings that arouse worry and leading to the spirit of adventures to make progress and arrive at the ways of reviving, creativity and modernism. The idea of prevailing of a certain culture or certain product in design depends on the given and available techniques, due to the fact that the computer and their artistic techniques become very important and vital to reinforce the image in the design. Thus, it is very necessary to link between these techniques and suitable way to reform the mentality by which the design will be reformed, from what has been said, (there has no utilization for the whole modern and available graphic techniques in the design proce

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Publication Date
Tue Mar 01 2016
Journal Name
Al-academy
Metaphor in product design: قيس والي عباس
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Addresses current research to the subject of metaphor as a field important in the design of industrial product, so it was a problem search: Does industrial product which is designed mainly to reflect the principle of metaphor role in receiving, and how the application of mechanisms theory correct as stipulated in institutions metaphor properly for this orientation in achieving those metaphors. What are the relations of reciprocity that influenced the establishment of the design and construction of the system for industrial product, the objectives of the research were standing on the interactive nature of the relations between the metaphor and the process of industrial product design? And identify strengths and weaknesses in the processes

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Publication Date
Mon Jan 08 2024
Journal Name
Al-academy
Mechanisms of creative action in print design
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In the midst of conflicts different intellectual and knowledge of production processes and circulation we need constant search for different levels of Innovation replenished with renewed need to develop solutions to various problems. Amid this conflict comes to mind a question about what salt creative mechanisms act in Graphic Design? Through this research is marked (creative mechanisms act in Graphic Design) strive to find solutions
to this question, as well as cognitive it Sarphi side modern and developmental study to a broader understanding of the subject. And across four seasons, which included the first chapter of the research problem and the need for him, and then came the second chapter includes theoretical framework goal Bemb

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Publication Date
Mon Jan 08 2024
Journal Name
Al-academy
Formal-semantic metaphor in print advertising design
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The research problem lay in the existing of this direct relation between the increasing and the big variety of the goods and the producing companies which mean the increase of the competition and the directing techniques of the commercial advertisings, which become spread everywhere and in an age characterized with the great varieties in the tests and the stances which requires the designers to seek designing accomplishments that are characterized with creativeness , seriousness and unsallity through the designer depending in constructing his / her texts and his/ her visual items on reference forms metaphors to achieve his / her designing purposes.
So the researcher through her primary flying study seek the identifying the manner of

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Publication Date
Wed Mar 15 2023
Journal Name
Al-academy
The Role of Context in Graphic Design
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The need for an intellectual understanding of the context from many aspects' dictates understanding the ways through which the graphic designer walks in simulating the intent of the design process and elevating it to levels of communicative perception that leads to communicating the idea to the recipient, and it is thus a need closely related to the context, if it is historical. Culturally or socially, and between the mechanisms of selecting and operating the elements and units of the graphic and design achievement. On this basis, the role of context in graphic design can be studied.

The research included four chapters, the first chapter of the research problem and the need for it, and the aim of the research was (discovering the

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Publication Date
Tue Aug 15 2023
Journal Name
Al-academy
Applications of Artificial Intelligence in Graphic Design
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If the Industrial Revolution has enabled the replacement of humans with machines, the digital revolution is moving towards replacing our brains with artificial intelligence, so it is necessary to consider how this radical transformation affects the graphic design ecosystem. Hence, the research problem emerged (what are the effects of artificial intelligence on graphic design) and the research aimed to know the capabilities and effects of artificial intelligence applications in graphic design, and the study dealt in its theoretical framework with two main axes, the first is the concept of artificial intelligence, and the second is artificial intelligence applications in graphic design. The descriptive approach adopted a method of content

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Publication Date
Sun Jun 11 2017
Journal Name
Al-academy
Processors Functional Design In Public Interior Spaces
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It is general known that any design in various fields such as the interior design in the field of spaces interior for the public and specific buildings that is concern about the use of humans resident , as well as other considerations relating to the organization of design elements and lines of locomotors activity and the validity of appropriate receiving to provide comfort and achieve the requirements of the position in the space of restaurants field of research.
The researcher choose the title of this study (processors design career in public spaces), the analytical study of the spaces of restaurants, as one of the public spaces that are running in their general environment of people in various strata , ages and other levels , whic

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