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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 Feb 24 2019
Journal Name
Iraqi Journal Of Physics
Design and evalution of a solar PV system
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PV connected systems are worldwide installed because it allows consumer to reduce energy consumption from the electricity grid. This paper presents the results obtained from monitoring a 1.1 kWp. The system was monitored for nine months and all the electricity generated was fed to the fifth floor for physics and renewable energy building   220 V, 50 Hz. Monthly, and daily performance parameters of the PV system are evaluated which include: average generated of system Ah per day, average system efficiency, solar irradiation around these months. The average generated kWh per day was 8 kWh/day, the average solar irradiation per day was 5.6 kWh/m2/day, the average inverter efficiency was 95%, the average modules efficien

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Publication Date
Wed Jun 14 2023
Journal Name
Al-academy
Fractal and its implications for industrial product design
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The current research dealt with the rapid development of industrial product design in recent times, and this development in the field of design led to the emergence of modern trends in many terms and theories to direct greater interest in the cognitive foundations of design and its relationship with the components of other natural sciences, and despite the impressive technological development, nature remains With its content of formative values and structural dimensions, it is the first source of inspiration and the source of all modern mathematical sciences and theories, as God made them tend towards organization to continue to provide us with endless inspiration. Hence, the fractional one, which is an important part of dedicating the d

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Publication Date
Wed Jun 12 2013
Journal Name
International Journal Of Computer Applications
Design and Implementation of a Practical FTTH Network
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Fiber-to-the-Home (FTTH) has long been recognized as a technology that provides future proof bandwidth [1], but has generally been too expensive to implement on a wide scale. However, reductions in the cost of electro-optic components and improvements in the handling of fiber optics now make FTTH a cost effective solution in many situations. The transition to FTTH in the access network is also a benefit for both consumers and service providers because it opens up the near limitless capacity of the core long-haul network to the local user. In this paper individual passive optical components, transceivers, and fibers has been put together to form a complete FTTH network. Then the implementation of the under construction Baghdad/Al

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Publication Date
Fri Dec 29 2017
Journal Name
Al-khwarizmi Engineering Journal
Design and Implementation of a Proposal Network Firewall
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In today's world, most business, regardless of size, believe that access to Internet is imperative if they are going to complete effectively. Yet connecting a private computer (or a network) to the Internet can expose critical or confidential data to malicious attack from anywhere in the world since unprotected connections to the Internet (or any network topology) leaves the user computer vulnerable to hacker attacks and other Internet threats. Therefore, to provide high degree of protection to the network and network's user, Firewall need to be used.

Firewall provides a barrier between the user computer and the Internet (i.e. it prevents unauthor

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Publication Date
Thu Oct 01 2009
Journal Name
Journal Of The College Of Languages (jcl)
ENGLISH FOR SPECIFIC PURPOSES (ESP) AND SYLLABUS DESIGN
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This research has discussed the origins of ESP, addressed key notions about ESP and examined issues in ESP syllabus design. The content of the paper was determined by a need identified based on my  experience as an ESL instructor designing and delivering the content-based language program - Language Preparation for the Cadets and Employment in the Iraqi  College of Police . These issues, where possible, have been supported by current and pertinent academic literature. It is my sincerest hope that these observations will lend insight into the challenges facing the ESL instructor acting as ESP syllabus developer.

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Publication Date
Thu Sep 15 2022
Journal Name
Al-academy
Interaction and functional structural transformation of product design
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The research discussed the propositions of functional structures and the requirements for their transformation according to the variables of use and human interaction through the variables of functions with one form products، multifunctional variables، and transforming form in one product. The patterns of user’s interaction with products were discussed through the variables of functional type، starting from defining the types of functions in the industrial product structures to: practical functions، which were classified into: informational functions، ergonomic functions، use، handling، comfort، global، anthropometric adaptation and physical postures. While the interaction variables were discussed according to the meaning fun

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Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
The Relations Of Design And The Role Of It Making The Idea For Fashion Design: فرات جمال العتابي
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Any design subject to a set of forces contributing to the establishment of relations working to strengthen the internal elements of the design; any imbalance in these elements can make a fragmented and weak design, thus preventing it from achieving the goal or performance. Poor performance can be attributed to various factors: the extent and function of the elements and principles in the design, realization of the idea, especially in fashion design.
Moreover, there are many aspects of a design that go into achieving the realization of the designer’s idea. The design utilizes a lot of stimulants by drawing attention to its design, which is consistent with the need for psychological and material individuals. In this research, we will

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Publication Date
Mon Jan 01 2024
Journal Name
Kafkas Universitesi Veteriner Fakultesi Dergisi
Assessment of In-vitro Cytotoxicity and In-ovo Virucidal Antiviral Efficacy of Various Plant Extracts and Bioactive Molecules
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Publication Date
Wed Jan 01 2025
Journal Name
Advances In Animal And Veterinary Sciences
Exposure to Environmental Perfluorooctanoic Acid (PFOA) Induced Hepatocellular Apoptosis and Alteration in Serum Biomarkers in Diabetic Guinea Pigs
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Publication Date
Sun Sep 07 2014
Journal Name
Baghdad Science Journal
Analysis of Fatty Acid Composition in the Seed and flower oil of Syrian Ligustrun Lucidum and olive oil
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The fatty acid composition in the seed and flower of Ligustrun lucidum and olive oil was studied by Gas Chromatography. Results showed that the main components of seed oil were Palmitic (C16:0) 5,893% ,Palmitolic acid (C16:1)0,398%, Steaeic (C18:0)2,911% ,Oleic (C18:1)74,984%,Linoleic (C18:2) 12,959%,and Linolenic (C18:3) 0,997%. The proportion of unsaturated fatty acid was above 89,338%, so the seed oil of L. lucidum ait belonged to unsaturated oil which possessed promising application. The components of flower oil were Palmitic (C16:0) 65,674% ,Palmitolic acid (C16:1)6,516%, Steaeic (C18:0)2,641% ,Oleic (C18:1)14,707%,Linoleic (C18:2) 3,113%,and Linolenic (C18:3) 2,70%. The proportion of unsaturated fatty acid and saturated fatty acid wa

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