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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 Feb 01 2021
Journal Name
Journal Of Engineering
Design narrow-band frequency amplifier (1.5GHz -1.6GHz) based on InGaP Heterojunction Bipolar Transistor (HBT) and GaAs HBT
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The research aims to design a narrow-band frequency drive amplifier (1.5GHz -1.6GHz), which is used to boost the transmitter amplifier's input signal or amplify the GPS, GlONASS signals at the L1 band.

The Power Amplifier printed circuit board (PCB) prototype was designed using InGaP HBT homogeneous technology transistor and GaAs Heterojunction Bipolar Transistor (HBT) transistor. Two models have been compared; one of the models gave 16dB gain, and the other gave 23dB when using an input power signal (-15dBm). The PCB consumes 2.4W of power and has a physical dimension of 11 x 4 cm.

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
Comparison between RSA and CAST-128 with Adaptive Key for Video Frames Encryption with Highest Average Entropy
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Encryption of data is translating data to another shape or symbol which enables people only with an access to the secret key or a password that can read it. The data which are encrypted are generally referred to as cipher text, while data which are unencrypted are known plain text. Entropy can be used as a measure which gives the number of bits that are needed for coding the data of an image. As the values of pixel within an image are dispensed through further gray-levels, the entropy increases. The aim of this research is to compare between CAST-128 with proposed adaptive key and RSA encryption methods for video frames to determine the more accurate method with highest entropy. The first method is achieved by applying the "CAST-128" and

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Publication Date
Fri Jul 30 2021
Journal Name
Iraqi Journal For Electrical And Electronic Engineering
EEG Motor-Imagery BCI System Based on Maximum Overlap Discrete Wavelet Transform (MODWT) and Machine learning algorithm
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The ability of the human brain to communicate with its environment has become a reality through the use of a Brain-Computer Interface (BCI)-based mechanism. Electroencephalography (EEG) has gained popularity as a non-invasive way of brain connection. Traditionally, the devices were used in clinical settings to detect various brain diseases. However, as technology advances, companies such as Emotiv and NeuroSky are developing low-cost, easily portable EEG-based consumer-grade devices that can be used in various application domains such as gaming, education. This article discusses the parts in which the EEG has been applied and how it has proven beneficial for those with severe motor disorders, rehabilitation, and as a form of communi

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Publication Date
Sat Oct 31 2020
Journal Name
International Journal Of Intelligent Engineering And Systems
Automatic Computer Aided Diagnostic for COVID-19 Based on Chest X-Ray Image and Particle Swarm Intelligence
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Publication Date
Fri May 17 2013
Journal Name
International Journal Of Computer Applications
Applied Minimized Matrix Size Algorithm on the Transformed Images by DCT and DWT used for Image Compression
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Publication Date
Sun Dec 01 2019
Journal Name
Al-khwarizmi Engineering Journal
An Experimental Study on Electrochemical Grinding Parameters on Hardness and Material Removal Rate for Stainless Steel 316
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Electrochemical Grinding (ECG) process is a mechanically assisted electrochemical process for material processing. The process is able to successfully machine electrically conducting harder materials at faster rate with improved surface finish and dimensional control. This research studies the effect of applied current, electrolyte concentration, spindle speed and the gap between workpiece and tool on hardness and material removal rate during electrochemical grinding for stainless steel 316. The characteristic features of the electrochemical grinding process are explored through Taguchi-design-based experimental studies. The better hardness can be obtained at 10 A of the current, 150 g/l of the electrolyte concentration, 0.3 mm of gap an

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Publication Date
Sun Jan 03 2010
Journal Name
Journal Of Educational And Psychological Researches
The non right behavior appearance for the kindergarten children and its relation with the kindergarten teaching style
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The kindergarten teacher play a role in fixing the children behavior so she must plant the value and the habits that make a positive behavior and accepted by the society so the teacher must know all the right educational psychological styles to fix the children behavior and make them accepted psychologically and socially so the problem of the research start from knowing the relation between the methods of dealing with the kindergarten’s teachers and the non right behavior appearance for the kindergarten children. The current research aims to measure the negative behavior appearance of the children of kindergarten and distinguish it according to (sex and levels) and to distinguish the most using styles by the teachers of kinderg

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Publication Date
Sun Sep 05 2010
Journal Name
Baghdad Science Journal
Composition operator induced by ?(z) = sz + t for which |s|?1, |t|<1 and |s|+|t|?1
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We study in this paper the composition operator that is induced by ?(z) = sz + t. We give a characterization of the adjoint of composiotion operators generated by self-maps of the unit ball of form ?(z) = sz + t for which |s|?1, |t|<1 and |s|+|t|?1. In fact we prove that the adjoint is a product of toeplitz operators and composition operator. Also, we have studied the compactness of C? and give some other partial results.

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Publication Date
Sat Jul 25 2026
Journal Name
Journal Of Physical Education
Some Biomechanical Limitation During Acceleration Phase and Its Relationship With (110) m Hurdles Achievement for Advance Runners
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Publication Date
Mon Oct 01 2012
Journal Name
Iraqi Journal Of Physics
Sttudy tthe oriienttattiion and diisttance ffacttors effffectts on tthe llower usablle ffrequency ((LUF)) over miiddlle eastt regiion
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In this research, the influence of the orientation and distance factors on the lowest usable frequency (LUF) parameter has been studied theoretically. The calculations of the (LUF) parameter have been made using the (VOACAP) international communication model for the connection links between the capital Baghdad and many other locations that distributed on different distances and directions over the Middle East region. The results shown in this study indicate there is a slight affection of the link direction (orientation) on the LUF parameter, while the influence of the distance factor is more significant on the values of the LUF parameter. The day/night effect appears for the long distance HF links (i.e. more than a 500 Km)

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