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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
Sat Dec 24 2022
Journal Name
Wasit Journal Of Pure Sciences
Synthesis of the integer FIR filters with short coefficient word length
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The integer simulation and development finite impulse response (FIR) filters taking into account the possibilities of their realization on digital integer platforms are considered. The problem statement and solution of multifunctional synthesis of digital FIR filters such a problem on the basis of the numerical methods of integer nonlinear mathematical programming are given. As an several examples, the problem solution of synthesis FIR-filters with short coefficient word length  has been given. The analysis of their characteristics is resulted. The paper discusses issues of modeling and synthesis of digital FIR filters with provision for the possibilities of their implementation on digital platforms with integer computation arithme

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Publication Date
Wed Sep 18 2024
Journal Name
Karbala International Journal Of Modern Science
Synthesis of ZnO: ZrO2 Nanocomposites Using Green Method for Medical Applications
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Publication Date
Mon Jul 01 2013
Journal Name
Journal Of Kerbala University
study the optimum conditions of synthesis AgNP by chemical reduction method
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Abstract :- In this paper, silver nanoparticles had been prepared by chemical reduction method. Many tests had been done to it such as UV-Visible spectrophotometer, XRD, AFM&SEM test. finally an attempt had been done to get the optimum condition to control the grain size of silver Nanoparticles by variation the heating period and other parameters which has an effect in silver Nanoparticles synthesis process. in this method we can get a silver nanoparticles in the size range from 52 to 97 nm.

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Publication Date
Sun Jun 04 2017
Journal Name
Baghdad Science Journal
Synthesis of Pure Nano semiconductor Oxide ZnO with Different AgNO3 Concentrations
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Zinc oxide nanoparticles sample is prepared by the precipitation method. This method involves using zinc nitrate and urea in aqueous solution, then (AgNO3) Solution with different concentrations is added. The obtained precipitated compound is structurally characterized by X-ray diffraction (XRD), Scanning electron microscopy (SEM), Atomic force microscopy (AFM) and Fourier transform infrared spectroscopy (FTIR). The average particle size of nanoparticles is around 28nm in pure, the average particle size reaches 26nm with adding AgNO3 (0.05g in100ml =0.002 M) (0.1g in100ml=0.0058M), AgNO3 (0.2g in 100ml=0.01M) was 25nm. The FTIR result shows the existence of -CO, -CO2, -OH, and -NO2- groups in sample and oxides (ZnO, Ag2O).and used an

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Publication Date
Wed Apr 30 2025
Journal Name
Iraqi Journal Of Science
Electrochemical Synthesis of Fe-doped TiO2 Nanotube for Gas Sensor Application
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Titanium dioxide (TiO2) nanotubes have gained particular interest as a material for gas sensors because of their vertical arrays, prepared by the anodization procedure. The presence of several oxygen vacancies in these nanotubes facilitates gas diffusion and provides additional active sites. This study examined the impact of voltages on the process of depositing iron nanoparticles onto arrays of TiO2 nanotubes (TNTs) for use as a gas sensor. The TNTs are manufactured using a straightforward and economical electrochemical anodization technique, specifically for gas sensor applications. By varying the deposition voltage (2-6 volts), ordered Fe-TNTs were efficiently manufactured using a simple two-step electrochemical process. It utili

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Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
The Physical Performance Of The Actor Within The Shows Of Anas Abdul Samad ( the play silence as the cry as a model): حليم هاتف جاسم
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The body has the ability to effect the audience in the the theatrical show , since he or she is transmitter , sender , seen and viewer of the humanitarian discourse as well the the images and connotations of the theatrical show, it is a tool of communication that substitutes for millions of spoken words, the modern schools of direction focused on the body language of the actor and gave it prominence in depicting facts by different connotations. The researcher studies the physical performance of the actor throughout focusing on the connotational dimensions of the body within the theatrical show , as well as the positioning of performative body within the modern schools of direction depending on the theatrical show (Rebuke ) of the Iraqi d

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Publication Date
Fri Nov 01 2019
Journal Name
Ecology, Environment And Conservation
Measurement of the concentration of lead in gasoline stations and in air battery factories and their effect of cytogenetic and hematological parameter in workers
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Publication Date
Tue Oct 30 2018
Journal Name
Journal Of Engineering
Study the Effect of Various Parameters on the Synthesis of ZSM-5 Zeolite
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ZSM-5 zeolite was synthesis under hydrothermal conditions at 175oC. The synthesis parameters have been investigated to find optimum synthesis method. Firstly, the crystallization time has been investigated to find the optimum crystallization time. Also, the ageing time was studied. The morphology, structure, and composition of the synthesized ZSM-5 zeolite were characterized using scanning electron microscopy (SEM), pH meter, viscometer, and X-ray powder diffraction (XRD). The bulk Si/Al ratio of ZSM-5 zeolite was in the range of 9.5—11.7. The synthesized ZSM-5 zeolite with appropriate ageing time could adjust crystal size and degree of the crystallinity. The crystal size of ZSM-5 zeolite obtained at an agei

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Publication Date
Mon Sep 11 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
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New complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Sun Dec 04 2011
Journal Name
Baghdad Science Journal
Use of cefoxitin as indicator for detection of Methicillin Resistant Staphylococcus aureus
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Rapid and accurate identification of Methicillin Resistant Staphylococcus aureus is essential in limiting the spread of this bacterium. The aim of study is the detection of Methicillin Resistant Staphylococcus aureus (MRSA) and determining their susceptibility to some antimicrobial agent. A total of fifty clinical Staphylococcus aureus, isolated from the nose of health work staff in surgery unit of Kalar general hospital and from ear of patients attended to the same hospital. The susceptibilities of isolates were determined by the disc diffusion method with oxacillin (1 ?g) and cefoxitin (30 ?g), and by the mannitol salt agar supplemented with cefoxitin (MSA-CFOX), susceptibilities of isolates to other antimicrobial agent were determined b

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