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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 Jul 09 2023
Journal Name
Journal Of Engineering
Comparison between Linear and Non-linear ANN Models for Predicting Water Quality Parameters at Tigris River
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In this research, Artificial Neural Networks (ANNs) technique was applied in an attempt to predict the water levels and some of the water quality parameters at Tigris River in Wasit Government for five different sites. These predictions are useful in the planning, management, evaluation of the water resources in the area. Spatial data along a river system or area at different locations in a catchment area usually have missing measurements, hence an accurate prediction. model to fill these missing values is essential.
The selected sites for water quality data prediction were Sewera, Numania , Kut u/s, Kut d/s, Garaf observation sites. In these five sites models were built for prediction of the water level and water quality parameters.

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Publication Date
Fri Apr 12 2019
Journal Name
Journal Of Economics And Administrative Sciences
Imported inflation ... concept, transmission channels, effects, and processors Iraq Case study for the period (1990-2015)
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This research aims to explain the effect of the imported inflation (which moves through the raise of global prices to Iraqi economy) over local prices, besides, the recognition the most important channels of imported inflation moving, its causes, effects, ways and policies that reduce the negative effects. To achieve the research aim, the deductive approach was adopted through using descriptive method to describe and determine phenomenon. The most important conclusion is that the research found out that there are two channels to transmission imported inflation in world. The first channel is the direct channel (prices) and the second channel is the indirect (income). The most important recommendation is to create sovereign fund (O

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Publication Date
Wed Jan 01 2020
Journal Name
Soil Science Society Of America Journal
Agroforestry, grass, biofuel crop, and row‐crop management effects on soil water dynamics for claypan landscapes
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Soil water use and water storage vary by vegetative management practices, and these practices affect land productivity and hydrologic processes. This study investigated the effects of agroforestry buffers (AB), grass buffers (GB), and biofuel crops (BC), relative to row crops (RC) on soil water use for a claypan soil in northern Missouri, USA. The experiment located at the Greenley Memorial Research Center included RC, AB, GB, and BC established in 1991, 1997, 1997, and 2012, respectively. Soil water reflectometer sensors installed at 5‐, 10‐, 20‐, and 40‐cm depths monitored soil water from April to November in 2017 and 2018. Results showed significant differences in weekly volumetric water content (VWC) among treatments for all fou

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Publication Date
Mon Feb 01 2021
Journal Name
Journal Of Physics: Conference Series
The Fear Effect on a Food Chain Prey-Predator Model Incorporating a Prey Refuge and Harvesting
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Abstract<p>In this paper, we investigate the impact of fear on a food chain mathematical model with prey refuge and harvesting. The prey species reproduces by to the law of logistic growth. The model is adapted from version of the Holling type-II prey-first predator and Lotka-Volterra for first predator-second predator model. The conditions, have been examined that assurance the existence of equilibrium points. Uniqueness and boundedness of the solution of the system have been achieve. The local and global dynamical behaviors are discussed and analyzed. In the end, numerical simulations are confirmed the theoretical results that obtained and to display the effectiveness of varying each parameter</p> ... Show More
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Publication Date
Thu Aug 04 2022
Journal Name
Contemporary Nurse
ICU nurses’ safety performance related to respect for safety and management commitment: A cross-sectional study
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Publication Date
Thu Jan 01 2026
Journal Name
Aip Conference Proceedings
Biogenic selenium nanoparticles by probiotics streptococcus salivarius and effect on oprM gene expression from Pseudomonas aeruginosa
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Publication Date
Fri Jan 31 2025
Journal Name
Passer Journal Of Basic And Applied Sciences
Enhanced Security Taxonomy for Fog-Enabled VANETs: A Comprehensive Survey on Attacks, Challenges, Applications and Architectures
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Vehicular Ad Hoc Networks (VANETs) are integral to Intelligent Transportation Systems (ITS), enabling real-time communication between vehicles and infrastructure to enhance traffic flow, road safety, and passenger experience. However, the open and dynamic nature of VANETs presents significant privacy and security challenges, including data eavesdropping, message manipulation, and unauthorized access. This study addresses these concerns by leveraging advancements in Fog Computing (FC), which offers lowlatency, distributed data processing near-end devices to enhance the resilience and security of VANET communications. The paper comprehensively analyzes the security frameworks for fog-enabled VANETs, introducing a novel taxonomy that c

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Publication Date
Fri Apr 14 2023
Journal Name
Journal Of Big Data
A survey on deep learning tools dealing with data scarcity: definitions, challenges, solutions, tips, and applications
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Abstract<p>Data scarcity is a major challenge when training deep learning (DL) models. DL demands a large amount of data to achieve exceptional performance. Unfortunately, many applications have small or inadequate data to train DL frameworks. Usually, manual labeling is needed to provide labeled data, which typically involves human annotators with a vast background of knowledge. This annotation process is costly, time-consuming, and error-prone. Usually, every DL framework is fed by a significant amount of labeled data to automatically learn representations. Ultimately, a larger amount of data would generate a better DL model and its performance is also application dependent. This issue is the main barrier for</p> ... Show More
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Publication Date
Mon Jul 01 2024
Journal Name
Journal Of Engineering
IoT-Based Low-Cost Smart Health Monitoring System using Raspberry Pi Pico W and Blynk Application
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في السنوات الأخيرة، أدى التقدم التكنولوجي في إنترنت الأشياء (IoT) وأجهزة الاستشعار الذكية إلى فتح اتجاهات جديدة وإعطاء حلول عملية في مختلف قطاعات الحياة. يتم التعرف على إنترنت الأشياء كتنولوجيا حديثة تربط بين مختلف انواع الشبكات. تم تحسين أنواع مختلفة من قطاعات الرعاية الصحية في المجال الطبي بناءً على هذه التكنولوجيا. أحد هذه القطاعات الهامة هو نظام مراقبة الصحة (HMS). تعتبر مراقبة المريض عن بعد لاسلكيًا وبت

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Publication Date
Wed Jul 27 2022
Journal Name
Journal Of Chemical Technology &amp; Biotechnology
Broad‐ranging review: configurations, membrane types, governing equations, and influencing factors on microbial desalination cell technology
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Abstract<p>Seawater might serve as a fresh‐water supply for future generations to help meet the growing need for clean drinking water. Desalination and waste management using newer and more energy intensive processes are not viable options in the long term. Thus, an integrated and sustainable strategy is required to accomplish cost‐effective desalination via wastewater treatment. A microbial desalination cell (MDC) is a new technology that can treat wastewater, desalinate saltwater, and produce green energy simultaneously. Bio‐electrochemical oxidation of wastewater organics creates power using this method. Desalination and the creation of value‐added by‐products are expected because of this ionic mov</p> ... Show More
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