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Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR, and HR-mass spectroscopy.

Results:

Compound S4 had a relatively high pharmacophore-fit score, indicating that it may have biological activity similar to the EGFR allosteric inhibitor reference, and it scored a relatively low ΔG against EGFR TK allosteric site, indicating a high likelihood of drug-receptor complex formation. Compound S4 was cytotoxic to the three cancer cell lines tested, particularly HCT-116 colorectal cancer cells, with an IC50 value comparable to Erlotinib. Compound S4 induced the intrinsic apoptotic pathway in HCT-116 cells by arresting them in the G2/M phase. All of the new derivatives, including S4, met the in silico requirements for EGFR allosteric inhibitory activity.

Conclusion:

Compound S4 is a promising EGFR tyrosine kinase allosteric inhibitor that warrants further research.

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Publication Date
Sun Jun 26 2022
Journal Name
International Journal Of Corrosion And Scale Inhibition
Synthesis of polysulfanilamide by electro polymerization and its corrosion protective properties on 316L stainless steel in 0.2 M HCl
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The electrochemical polymerization of the monomer sulfanilamide (SAM) in an aqueous solution at room temperature produces polysulfanilamide (PSAM). The Fourier Transform Infrared spectroscopy (FTIR) was used to investigate the properties of the prepared polymer layer that generated on the stainless steel (St.S) surface (working electrode) and Atomic Force Microscope (AFM) was used to characterize the morphology, topology, and detailed surface structure of polymer layer that generated on the surface. The corrosion behavior of uncoated and coated St.S were evaluated by using the electrochemical polarization method in a 0.2 M HCl solution and a temperature range of 293–323 K, the anticorrosion action of the polymer coating on stainless steel

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Publication Date
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Anticancer Activity of Chitosan Schiff Base / PVP Gold Nano Composite in Treating Esophageal Cancer Cell Line
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In the present paper, chitosan Schiff base has been synthesized from chitosan’s reaction with the salicyldehyde. The AuNPs was manufacture by extract of onion peels as a reducing agent. The Au NPs that have been prepared were characterized through the UV-vis spectroscopy, XRD analyses and SEM microscopy. The polymer blends of the chitosan Schiff base / PVP has been prepared through using the approach of solution casting. Chitosan Schiff base / PVP Au nano-composites was prepared. Nano composites and polymer blends have been characterized by FTIR which confirm the formation of Schiff base by revealing a new band of absorption at 1651cm-1 as a result of the (C=N) imine group. SEM, DSC and TGA confirms the thermal stability of

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Publication Date
Sat May 20 2023
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Anticancer Activity of Chitosan Schiff Base / PVP Gold Nano Composite in Treating Esophageal Cancer Cell Line
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In the present paper, chitosan Schiff base has been synthesized from chitosan’s reaction with the salicyldehyde. The AuNPs was manufacture by extract of onion peels as a reducing agent. The Au NPs that have been prepared were characterized through the UV-vis spectroscopy, XRD analyses and SEM microscopy. The polymer blends of the chitosan Schiff base / PVP has been prepared through using the approach of solution casting. Chitosan Schiff base / PVP Au nano-composites was prepared. Nano composites and polymer blends have been characterized by FTIR which confirm the formation of Schiff base by revealing a new band of absorption at 1651cm-1 as a result of the (C=N) imine group. SEM, DSC and TGA confirms the thermal stability of the pr

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Publication Date
Tue Nov 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Adoption of Membership Level for Critical Activities In Knowledge Chain Model Building An Investigation Analytical Study Depending on Fuzzy Logic Architecture for Organizations Pushed by Knowledge
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Abstract

   The aim of this research is to concentrate on the of knowledge management activities, initial activities: (Acquisition, Selection, Generation, Assimilation, Emission) knowledge, and support activities: (Measurement, Control, Coordination, Leadership) that is manipulate and controlling in achieving knowledge management cases in organization, that’s is leads to  knowledge chain model, then determining the level of membership for these activities to knowledge chain model in a sample of Iraqi organization pushed by knowledge (Universities). The research depends on check list for gaining the data required, theses check list designed by apparently  in diagnosing research dimensions and measurem

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Publication Date
Wed Jan 01 2014
Journal Name
Journal Of The College Of Languages (jcl)
Tennessee Williams: Memories as symbols in The Glass Menagerie
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The Glass Manegerie is a metaphor, which is one of the greatest plays  of great writer Williams. The play talks about  the poor people in society and how try to escape this group of people from the real world to get rid of the hardness of this tuff reality and live in a fantasy world that is much like the glass where the world is very weak this world is acting by Laura, she is  owner of these animals breakable glass where it's weak and unable to defend itself as well as the mother Amanda  is a very selfish never think about her children but only herself.

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Publication Date
Sat Feb 01 2025
Journal Name
Iop Conference Series: Earth And Environmental Science
Chitosan as an Aflatoxin Inhibitor in Local Fish Feed
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Abstract<p>The current research attempts to find a feed additive that enhances fish growth and eliminate toxins generated from fungi and mold, which are found in improperly manufactured and stored feed, while ensuring the safety of these fish meat for the consumer. Therefore, the organic properties of chitosan powder were examined in order to determine its impact on maturation of young <italic>Cyprinus carpio</italic>. Chitosan was tested in three samples of feedings at three concentrations: CH1 7gm/1kg fish feed, CH2 10gm/1kg, and CH3 15gm/1kg carp fish feed. The results showed that the third parameter, 15gm CH3 chitosan/kg of feed, was superior to the other parameters, having a highl</p> ... Show More
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Publication Date
Wed Sep 01 2021
Journal Name
Journal Of Engineering
Spike neural network as a controller in SDN network
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The paper proposes a methodology for predicting packet flow at the data plane in smart SDN based on the intelligent controller of spike neural networks(SNN). This methodology is applied to predict the subsequent step of the packet flow, consequently reducing the overcrowding that might happen. The centralized controller acts as a reactive controller for managing the clustering head process in the Software Defined Network data layer in the proposed model. The simulation results show the capability of Spike Neural Network controller in SDN control layer to improve the (QoS) in the whole network in terms of minimizing the packet loss ratio and increased the buffer utilization ratio.

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Publication Date
Thu Jul 13 2023
Journal Name
International Journal Of Research In Social Sciences &amp; Humanities
Subject Review: Blogs as Learning Tools in EFL Classrooms
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Blogs have emerged as a powerful technology tool for English as a Foreign Language (EFL) classrooms. This literature review aims to provide an overview of the use of blogs as learning tools in EFL classrooms. The study examines the benefits and challenges of using blogs for language learning and the different types of blogs that can be used for language learning. It provides suggestions for teachers interested in using blogs as learning tools in their EFL classrooms. The findings suggest that blogs are a valuable and effective tool for language learning, particularly in promoting collaboration, communication, and motivation.

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Publication Date
Mon Mar 01 2010
Journal Name
Al-khwarizmi Engineering Journal
Synthetic Sacks as Reinforced Fibers in the Thermosetting Composites
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This study was carried out to investigate the preparation of thermosetting polymeric blend consisting of three adhesive types, namely: epoxy, polyvinyl formal (PVF) and unsaturated polyester. Both of epoxy and PVF were used as a matrix-binder at fixed weight. Whilst unsaturated polyester was used at different weights and added to the matrix so as to produce prepared epoxy-PVF-unsaturated polyester blend. Several experiments were performed at different operating conditions, mixing speed and time at room temperature to identify the most favorable operating conditions. The optimum mixing speed and mixing time for the prepared blend were 500rpm and 5 minutes respectively.

      Solid wastes-synthetic sack fib

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Publication Date
Fri Nov 01 2024
Journal Name
Process Safety And Environmental Protection
Optimized ensemble deep random vector functional link with nature inspired algorithm and boruta feature selection: Multi-site intelligent model for air quality index forecasting
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