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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 Jul 01 2020
Journal Name
Plant Archive
A new species of genus stachys L. (Lamiaceae) in Iraq
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Scopus
Publication Date
Mon Jan 01 2018
Journal Name
Al–bahith Al–a'alami
The Communicative Integration in New Media: Building a Communicative Model
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The internet, unlike other traditional means of communication, has a flexibility to stimulate the user and allows him to develop it. Perhaps, the reason for the superiority of the internet over other traditional means of communication is the possibility of change and transmission from one stage to another in a short period. This means that the internet is able to move from the use to the development of the use and then the development of means and innovation as the innovation of the internet is a logical product of the interaction of the user with the network. The internet invests all the proposals and ideas and does not ignore any even if it is simple. This is represented in social networking sites which in fact reflects personal emotio

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Crossref
Publication Date
Wed Jan 02 2019
Journal Name
Journal Of The College Of Languages (jcl)
The Victorian Society’s Fear of the New Woman in Bram
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Nineteenth century Gothic literature was deeply concerned with the threats against masculinity. Perhaps one of the most important changes that happened at that time was the emergence of the New Woman model which posed a great threat against masculinity and the male role in the Victorian society. Bram Stoker’s Dracula (1897) portrays female characters who embody this transition in female roles from the domestic wife to the New Woman. This paper focuses on the female characters Mina Murray and Lucy Westenra, their roles in their society, and the different fates they face at the end of the novel, with special focus on Mina’s transformation to the model of the New Woman.

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Publication Date
Tue Jul 01 2003
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
NEW RECORDS OF SOME MITE SPECIES INHABITING SOIL IN BAGHDAD
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The soil acari fauna of Citrus orchards of Baghdad in Jadiriya area was studied in a total
of forty-eight samples. Twenty-two species were recorded during the present study of which
eight species were first records to Iraq. The ordinal composition of the soil acari fauna was
predominantly Mesostigmata.
This fauna represents diverse trophic groups. The most abundant groups were the
predacious and the Microphytophagus, while the less abundant groups were the predacious/
Microphytophagus, Macrophytophagus, and Panaphytophagus. The most abundant and
frequent species were Rhizoglyphus sp. Tyrophagus putrescentiea (Scrank), Pachylaelaps
longisetis Halbt. and Stratiolaelaps miles Berl.

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Publication Date
Wed Feb 01 2023
Journal Name
Baghdad Science Journal
Some New Fixed Point Theorems in Weak Partial Metric Spaces
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The main objective of this work is to introduce and investigate fixed point (F. p) theorems for maps that satisfy contractive conditions in weak partial metric spaces (W.P.M.S), and give some new generalization of the fixed point theorems of Mathews and Heckmann. Our results extend, and unify a multitude of (F. p) theorems and generalize some results in (W.P.M.S). An example is given as an illustration of our results.

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Publication Date
Wed Jul 30 2025
Journal Name
Methodsx
New Modifications of ADM with Applications in Kind of PDEs
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This paper presents seven modified Adomian Decomposition Method (ADM) techniques for efficiently solving initial value problems, especially those involving non-homogeneous and nonlinear differential equations. While the classical ADM is effective for linear homogeneous cases, it has difficulties solving more complex problems. The proposed modifications—from MADM1 to MLADM—include Maclaurin and Taylor expansions, Laplace transforms, and single-step iterations.• These modifications enhance convergence, reduce complexity, and improve accuracy.• Each method offers specific advantages, such as accelerating convergence (MADM2, RADM4), simplifying computation (TSADM5), and achieving higher accuracy (MLADM).• Numerical examples confirm th

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Publication Date
Mon Sep 03 2018
Journal Name
Al-academy
A new vision for the classic in contemporary fashion designResearch
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        fashion designers who have benefited greatly from the mobilization of ancient aesthetic ideas in the heritage of the people and guaranteed in their productions so that there is no change In the aesthetic value created by the designers of the research in the ancient heritage to find new signs that reflect the connection of man to the present as the aesthetic value of all the man created by the designs of fabrics and fashion through the ages      The problem of research was determined in the absence of a precise understanding of the nature of classical thought in fashion and the absence of a clear perception of the sustainability of this thought in contemporary fashion. He

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Publication Date
Thu Jun 27 2019
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
TWO NEW RECORDS OF THE GENUS APHODIUS ILLIGE, 1798 (COLEOPTERA: APHODIIDAE) IN IRAQTWO NEW RECORDS OF THE GENUS APHODIUS ILLIGE, 1798 (COLEOPTERA: APHODIIDAE) IN IRAQ
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    In this study, the dung beetles Aphodius (Bodilus) ictericus (Laicharting, 1781) and Aphodius (Planolinellus) vittatus Say, 1825 which belongs to the family of Aphodiidae (Order: Coleoptera) are redscribed here as to being found for the first time in Iraq.

 

    The specimens were collected from different regions in the middle of Iraq; the main diagnostic characters and some morphological features of males were drawn and pictured.

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Publication Date
Tue Dec 15 2020
Journal Name
Al-academy
Acculturation and its Evolutionary Tendency in the Design of the Prayer Space Elements / Niche – A model: آلاء طالب كريم
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The peculiarity of worship spaces in the Islamic architecture is evident by its symbolic connotations with doctrinal connections, thus the niche has a major status in that symbolic connotation, which transformed due to the cultural interaction from a rock on the wall directed towards Mecca into an element of integrated structural entity with performative and aesthetic characteristics. The spread of the Islamic religion contributed to subjecting it to a design acculturation process, thus the problem of the research was raised by the following question: has the evolutionary tendency of acculturation been able to effect a major transformation in the niche design? The research aims at identifying the design acculturation and its translation

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Publication Date
Wed Dec 31 2025
Journal Name
Modern Sport
The Contribution of Design Thinking to Reducing Excessive Sensitivity to Criticism Among Athletes in Selected Track and Field Events
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