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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
Tue Jan 01 2019
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability: Tmrees19gr
Improvement photoluminescence of nematic liquid crystal doped with gold nanoparticles
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Publication Date
Wed Jun 11 2003
Journal Name
Iraqi Journal Of Laser
Q- Switched Nd:YAG Laser Annealing of Phosphorus Diffused Silicon Photodiodes
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Improvement of optoelectrical characteristics of phosphorus diffused silicon photodiodes by Q-switched Nd:YAG laser pulses was investigated. Laser pulses have dissolved the precipitation of phosphorus resulted during thermal diffusion process. The experimental data show that responsivity higher than (0.32 A/W) at 850 nm can be achieved after laser annealing with (1.5 MW/cm2) for 6 shots.

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Publication Date
Tue Sep 15 2020
Journal Name
Al-academy
Impact of Cranbrook on Graphic Design: راقي صباح نجم الدين
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  Empirical research in the disciplines of art and design has started to escalate and gather consideration within the academic community over the past few decades. However, still, graphic design tends to be a topic extremely under-researched by scholarly persons. Profound research in the field of graphic design extends far beyond the works produced by the designer himself (Khoury, 2009, p.844). In order to develop a clear insight, one needs to delve deep into the subcategories that the diverse field of graphic design is comprised of, including illustration, typography, interaction design, branding and even the impact of notable, eminent institutes from around the world that have taken the budding artists for quite a long time (Walke

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Publication Date
Wed Jun 17 2015
Journal Name
جامعة المستنصرية
study of some aspect on Iraqi children with Atopic Dermatitis
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Publication Date
Thu Apr 18 2024
Journal Name
Geomatics And Environmental Engineering
Error Analysis of Stonex X300 Laser Scanner Close-range Measurements
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This research reports an error analysis of close-range measurements from a Stonex X300 laser scanner in order to address range uncertainty behavior based on indoor experiments under fixed environmental conditions. The analysis includes procedures for estimating the precision and accuracy of the observational errors estimated from the Stonex X300 observations and conducted at intervals of 5 m within a range of 5 to 30 m. The laser 3D point cloud data of the individual scans is analyzed following a roughness analysis prior to the implementation of a Levenberg–Marquardt iterative closest points (LM-ICP) registration. This leads to identifying the level of roughness that was encountered due to the range-finder’s limitations in close

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Publication Date
Sun Jan 10 2016
Journal Name
British Journal Of Applied Science & Technology
The Effect of Classification Methods on Facial Emotion Recognition ‎Accuracy
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The interests toward developing accurate automatic face emotion recognition methodologies are growing vastly, and it is still one of an ever growing research field in the region of computer vision, artificial intelligent and automation. However, there is a challenge to build an automated system which equals human ability to recognize facial emotion because of the lack of an effective facial feature descriptor and the difficulty of choosing proper classification method. In this paper, a geometric based feature vector has been proposed. For the classification purpose, three different types of classification methods are tested: statistical, artificial neural network (NN) and Support Vector Machine (SVM). A modified K-Means clustering algorithm

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Publication Date
Sat Apr 01 2017
Journal Name
Al–bahith Al–a'alami
The Bahraini Daily Press Coverage of Women Issues): (Analytical Study
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This research is an attempt to assess the extent of coverage given by the Bahrain daily press to Women and related issues. It attempts to determine how important the issues of the Women issues were covered in the Daily Press and whether the press has given enough attention to the Women issues.
The research was conducted by analyzing the coverage “AkhbarAlKhaleej” Daily newspaper gave the Women issues during the period of this study.
Thus, this study aims at assessing the degree to which the Bahraini daily newspapers have dealt with the Women issues. The researcher analyzed the contents of the Bahraini press, “AKHBAR ALKHALEEJ” daily newspaper during 2014, as Bahraini press coverage seems to be stable, and more balanced and

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Publication Date
Sun Feb 01 2015
Journal Name
Journal Of Engineering
Design a Multi-Choice Fuzzy Control System of the Greenhouse
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Applications of nonlinear, time variant, and variable parameters represent a big challenge in a conventional control systems, the control strategy of the fuzzy systems may be represents a simple, a robust and an intelligent solution for such applications.

This paper presents a design of fuzzy control system that consists of three sub controllers; a fuzzy temperature controller (FC_T), a fuzzy humidity controller (FC_H) and a ventilation control system; to control the complicate environment of the greenhouse (GH) using a proposed multi-choice control system approach. However, to reduce the cost of the crop production in the GH, the first choice is using the ventilation system to control the temperature and humidit

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Publication Date
Sun Sep 30 2012
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
The Control of Non Isothermal CSTR Using Different Controller Strategies
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In all process industries, the process variables like flow, pressure, level, concentration
and temperature are the main parameters that need to be controlled in both set point
and load changes.
A control system of propylene glycol production in a non isothermal (CSTR) was
developed in this work where the dynamic and control system based on basic mass
and energy balance were carried out.
Inlet concentration and temperature are the two disturbances, while the inlet
volumetric flow rate and the coolant temperature are the two manipulations. The
objective is to maintain constant temperature and concentration within the CSTR.
A dynamic model for non isothermal CSTR is described by a first order plus dead
time (FO

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Publication Date
Sat Oct 28 2023
Journal Name
Baghdad Science Journal
Numerical Modeling of Renal Ionic Equilibrium for Implantable Kidney Applications
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The human kidney is one of the most important organs in the human body; it performs many functions
and has a great impact on the work of the rest of the organs. Among the most important possible treatments is
dialysis, which works as an external artificial kidney, and several studies have worked to enhance the
mechanism of dialysate flow and improve the permeability of its membrane. This study introduces a new
numerical model based on previous research discussing the variations in the concentrations of sodium,
potassium, and urea in the extracellular area in the blood during hemodialysis. We simulated the differential
equations related to mass transfer diffusion and we developed the model in MATLAB Simu

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