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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 Jul 01 2024
Journal Name
Iop Conference Series: Earth And Environmental Science
Refinement of Internal-Combustion Engine Oil Properties Via Magnetic Flux
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Abstract<p>To verify the influence of magnetic flux on the characteristics of SAE 10W-30 gasoline engine oil when the engine oil is exposed to different magnetic fluxes 0, 6, 9, and 13 Volt. The following oil characteristics were measured: viscosity at 40 and 100 °C, and total acid number (TAN) mg KOH/g. The research was carried out in a completely randomized design with three replications for each treatment under the 5% probability level to compare the means of the treatments. The results of the experiment showed that there were significant differences in the studied properties when the engine oil was exposed to the above magnetic fluxes and, inversely, especially the magnetic flux of 13 Volt,</p> ... Show More
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Publication Date
Fri Apr 05 2013
Journal Name
Journal Of Intelligent Material Systems And Structures
Increasing the power of piezoelectric energy harvesters by magnetic stiffening
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A piezoelectric cantilever beam with a tip mass at its free end is a common energy harvester configuration. This article introduces a new principle of designing such a harvester that increases the generated power without changing the resonance frequency of the harvester: the attraction force between two permanent magnets is used to add stiffness to the system. This magnetic stiffening counters the effect of the tip mass on the efficient operation frequency. Five set-ups incorporating piezoelectric bimorph cantilevers of the same type in different mechanical configurations are compared theoretically and experimentally to investigate the feasibility of this principle: theoretical and experimental results show that magnetically stiffened harve

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Publication Date
Sun Feb 01 2026
Journal Name
Applied Acoustics
Development of an acoustic vacuum gauge for low-pressure measurement
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Publication Date
Sun Mar 04 2018
Journal Name
Baghdad Science Journal
Enhanced Photocurrent of Titania Nanotube Photoelectrode Decorated with CdS Nanoparticles
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In this work, CdS/TiO2 nanotubes composite nanofilms were successfully synthesized via electrodeposition technique. TiO2 titania nanotube arrays (NTAs) are commonly used in photoelectrochemical cells as the photoelectrode due to their high surface area, excellent charge transfer between interfaces and fewer interfacial grain boundaries. The anodization technique of titanium foil was used to prepare TiO2 NTAs photoelectrode. The concentration of CdCl2 played an important role in the formation of CdS nanoparticles. Field emission scanning electron microscopy (FESEM) shows that the CdS nanoparticles were well deposited onto the outer and inner of nanotube at 40 mM of CdCl2. X-ray diffraction (XRD) and energy dispersive X-ray (EDX) analyses wer

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Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
The Effect of Speaking Strategies on Iraqi EFL College Students
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The present study deals with the effect of teaching speaking Strategies (SS) on
EFL Iraqi College students. The use of speaking strategies not only solves learners’
communication problems, but also enhances the learner’s interaction in target language,
and improves their oral proficiency .The aim of the study is to find out the effect of
teaching SS used by EFL College students .The learner of the first stage is population of
the study at the Department of English, College of Education /Ibn-Rushd .The sample
consists of (60) students distributed on experimental group(A) as well as control
group(B) each group contains (30) students . In order to achieve the aim of the study,
questionnaire has been constructed t

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Publication Date
Mon Jan 01 2018
Journal Name
International Journal Of Medical Research & Health Sciences
Non-Surgical Treatment of Gingival Recession by Platelet-Rich Plasma
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Publication Date
Sat Jan 31 2015
Journal Name
International Journal Of Research In Applied, Natural And Social Sciences
The Influence of Premenopausal Simple Hysterectomy on Bone Mass Density
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Publication Date
Tue Oct 02 2018
Journal Name
Iraqi Journal Of Physics
Frustrated total internal reflection of newton rings multiple beam interference
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Frustrated Total Internal Reflection FTIR phenomenon is manifested employing Newton‟s rings setup generated via a coherent light beam of a laser diode ( . All concentric bright and dark rings, except the central bright spot, were noticed to recede (disappear) when the incident angle exceeded the critical angle of 41o.
It was also shown that the current setup has proven its applicability for other tests and can give convenient results that conform with theory. Neither the concept nor the design is beyond what can be realized in an undergraduate laboratory. However, technical improvements in mounting the prism - lens may be advisable. As an extension of the experiments, the effect can be studied using hollow prism filled with liquids

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Publication Date
Thu Jan 30 2020
Journal Name
Journal Of Engineering
The Optimum Reservoir Performance of Nahr Umr/Ratawi Oil Field
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Reservoir study has been developed in order to get a full interesting of the Nahr Umr formation in Ratawi oil field. Oil in place has been calculated for Nahr Umr which was 2981.37 MM BBL. Several runs have been performed to get matching between measured and calculated of oil production data and well test pressure. In order to get the optimum performance of Nahr Umr many strategies have been proposed in this study where vertical and horizontal wells were involved in addition to different production rates. The reservoir was first assumed to be developed with vertical wells only using production rate of (80000–125000) STB/day. The reservoir is also proposed to produce using horizontal wells besides vertical wells with production rat

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Publication Date
Thu Oct 01 2009
Journal Name
2009 Ieee Symposium On Industrial Electronics &amp; Applications
ITTW: T-way minimization strategy based on intersection of tuples
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