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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
Mon Oct 23 2023
Journal Name
Journal Of Optics
Single mode optical fiber sensor based on surface plasmon resonance for the detection of the oil aging for the electrical transformers
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This work presents a novel technique for the detection of oil aging in electrical transformers using a single mode optical fiber sensor based on surface plasmon resonance (SPR). The aging of insulating oil is a critical issue in the maintenance and performance of electrical transformers, as it can lead to reduce insulation properties, increase risk of electrical breakdown, and decrease operational lifespan. Many parameters are calculated in this study in order to examine the efficiency of this sensor like sensitivity (S), signal to noise ratio (SNR), resolution (refractive index unit) and figure of merit (FOM) and the values are for figure of merit is 11.05, the signal to noise ratio is 20.3, the sensitivity is 6.63, and the resolution is 3

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Publication Date
Sun Jan 01 2017
Journal Name
Food And Nutrition Sciences
Optimization of Culture Conditions to Produce Phytase from <i>Aspergillus tubingensis SKA</i>
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The effects of nutrients and physical conditions on phytase production were investigated with a recently isolated strain of Aspergillus tubingensis SKA under solid state fermentation on wheat bran. The nutrient factors investigated included carbon source, nitrogen source, phosphate source and concentration, metal ions (salts) and the physical parameters investigated included inoculum size, pH, temperature and fermentation duration. Our investigations revealed that optimal productivity of phytase was achieved using wheat bran supplemented with: 1.5% glucose. 0.5% (NH4)2SO4, 0.1% sodium phytate. Additionally, optimal physical conditions were 1 × 105 spore/g substrate, initial pH of 5.0, temperature of fermentation 30˚C and fermentation dura

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Publication Date
Mon Aug 25 2025
Journal Name
مجلة كلية التربية
A Multi-modal Critical Discourse Analysis of Selected English Political Cartoons تحليل خطاب نقدي متعدد الوسائط لرسوم كاريكاتورية سياسية إنجليزية مختارة
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This study analyses six political cartoons selected based on their relevance to current Iraqi political issues, specifically the period between 2005 and 2015, from American online newspapers (calgecartooms.com). The selection criteria included the cartoons' satirical elements, visual rhetoric, and their ability to engage with themes such as power dynamics, social issues, and public opinion. It sheds light on how these cartoons can function as mediators of meanings between the cartoonists and the readers. The data is examined using multimodal discourse analysis (MDA), which combines language study with the analysis of other visual elements, like colors, gestures, and images, to understand meaning (O’Halloran et al., 2011). The Visual Socia

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Publication Date
Sat Nov 30 2024
Journal Name
Asia Pacific Journal Of Molecular Biology And Biotechnology
Random amplified polymorphic DNA-based polymerase chain reaction is an effective tool to examine the genotoxic effects of some food colors
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A large number of natural or synthetic dyes have been removed from both national and international lists of permitted food colors because of their mutagenic or carcinogenic activity. Therefore, this study aimed to use the Random Amplified Polymorphic DNA-Based Polymerase Chain Reaction (RAPD-PCR) assay as a feasible method to evaluate the ability of some food colors as genotoxin-induced DNA damage and mutations. Lactiplantibacillus plantarum was used as a bioindicator to determine the genotoxic effects by RAPD-PCR using M13 primer after treatment with some synthetic dyes currently used as food color additives, including Sunset Yellow, Carmoisine, and Tartrazine. Besides qualitative analysis, the bioinformatic GelJ software was used for clus

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Publication Date
Thu Sep 01 2016
Journal Name
Chem Istry & Chem Ical Technology
SYN TH ESIS, CH ARACTERIZATION AN D AN TIM ICROBIAL ACTIVITY OF N EW N UCLEOSIDE AN ALOGUES FROM BEN ZOTRIAZOLE
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Novel derivatives of 1-(´1, ´3, ´4, ´6-tetra benzoyl-β-D-fructofuranosyl)-1H- benzotriazole and 1-(´1, ´3, ´4, ´6-tetra benzoyl-β-D-fructofuranosyl)-1H- benzotriazole carrying Schiff bases moiety were synthesised and fully characterised. The protection of D- fructose using benzoyl chloride was synthesized, followed by nucleophilic addition/elimination between benzotria- zole and chloroacetyl chloride to give 1-(1- chloroacetyl)- 1H-benzotriazole. The next step was condensation reaction of protected fructose and 1-(1-chloroacetyl)-1H- benzotriazole producing a new nucleoside analogue. The novel nucleoside analogues underwent a second conden- sation reaction with different aromatic and aliphatic amines to provide new Schiff b

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Publication Date
Sun Jun 30 2024
Journal Name
International Journal Of Intelligent Engineering And Systems
Enhancement of the Blood Glucose Level for Diabetic Patients Based on an Adaptive Auto-Tuned PID Controller via Meta-Heuristic Methods
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Publication Date
Sun Jul 09 2023
Journal Name
Journal Of Engineering
A Comparative Study of Various Intelligent Algorithms Based Nonlinear PID Neural Trajectory Tracking Controller for the Differential Wheeled Mobile Robot Model
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This paper presents a comparative study of two learning algorithms for the nonlinear PID neural trajectory tracking controller for mobile robot in order to follow a pre-defined path. As simple and fast tuning technique, genetic and particle swarm optimization algorithms are used to tune the nonlinear PID neural controller's parameters to find the best velocities control actions of the right wheel and left wheel for the real mobile robot. Polywog wavelet activation function is used in the structure of the nonlinear PID neural controller. Simulation results (Matlab) and experimental work (LabVIEW) show that the proposed nonlinear PID controller with PSO
learning algorithm is more effective and robust than genetic learning algorithm; thi

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Publication Date
Mon Aug 05 2024
Journal Name
Food And Bioprocess Technology
Development of an Innovative Reinforced Food Packaging Film Based on Corn Starch/Hydroxypropyl Methylcellulose/Nanocrystalline Cellulose Incorporated with Nanogel Containing Quercetin
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Publication Date
Wed Jun 01 2022
Journal Name
Analytical Methods In Environmental Chemistry Journal
Design a continuous microfluidic flow cell for turbidimetric-flow injection technology: A new approach for routine analysis of active pharmaceutical formulations
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Publication Date
Mon Mar 07 2022
Journal Name
Journal Of Educational And Psychological Researches
The Effect of Teaching According to the Augmented Reality Technique on theVisual Thinking Skills to Scientific Fifth-Grade Students for Biology
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The research aims to identify the effect of teaching according to the augmented reality on the technique of the visual thinking skills among scientific fifth-grade students in a biology course. In order to achieve the goal of the research, the researcher adopted the experimental approach with the partial set of the two equal groups with the dimensional test of visual thinking skills, The research population represented all the scientific students of the fifth grade for morning government schools affiliated to the General Directorate of Education of Baghdad / Karkh II, alshakerin preparatory for boys was chosen intentionally, in which two groups were chosen for this study, one group is chosen randomly as the control group via lottery, whe

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