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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
Fri Mar 01 2019
Journal Name
Iraqi Journal Of Physics
Wear rate of epoxy resin reinforced with multi walls carbon nanotubes
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In this study, nanocomposites have been prepared by adding
multiwall carbon nanotubes (MWCNTs) with weight ratios (0, 2, 3,
4, 5) wt% to epoxy resin. The samples were prepared by hand lay-up
method. Influence of an applied load before and after immersion in
sodium hydroxide (NaOH) of normality (0.3N) for (15 days) at
laboratory temperature on wear rate of Ep/MWCNTs
nanocomposites was studied. The results showed that wear rate
increases with increasing the applied load for the as prepared and
immersed samples and after immersion. It was also found that epoxy
resin reinforced with MWCNTs has wear rate less than neat epoxy.
The sample (Ep + 5wt% of MWCNTs) has lower wear rate. The
immersion effect in base so

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Publication Date
Sat Mar 30 2013
Journal Name
College Of Islamic Sciences
 The choices of Ibn Muqasim (354 AH) from the Qur’anic readings
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This research examines aspects of Imam Al-Qurtubi's efforts in matters related to the topics of faith that he dealt with in his interpretation (the provisions of the provisions of the Qur’an); and it has been shown that Imam Al-Qurtubi in most of the doctrinal issues dealt with in his interpretation approximates the doctrine of the Sunnis of Ash'aris, Maturids and people of impact. He had responses to some of the teams, such as stereoscopic, karami, and Mu'tazilite, reinforcing the responses with transfer and mental evidence.
    It was found that Imam Al-Qurtubi says that there is an increase in faith and a decrease in it, that the increase is through actions (so obedience increases and decreases in sin) and that the

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Publication Date
Mon Jun 01 2020
Journal Name
Journal Of Engineering
Evaluating Asphalt Concrete Properties by the Implementation of Ultrasonic Pulse Velocity
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In past years, structural pavement solution has been combined with destructive testing; these destructive methods are being replaced by non-destructive testing methods (NDT). Because the destructive test causes damage due to coring conducted for testing and also the difficulty of adequately repairing the core position in the field. Ultrasonic pulse velocity was used to evaluate the strength and volumetric properties of asphalt concrete, of binder course. The impact of moisture damage and testing temperature on pulse velocity has also been studied. Data were analyzed and modeled. It was found that using non-destructive testing represented by pulse velocity could be useful to predict the quality of asphalt c

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Publication Date
Sat Jul 22 2023
Journal Name
Journal Of Engineering
Removal of Boron from Simulated Iraqi Surface Water by Electrocoagulation Method
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The removal of boron from aqueous solution was carried out by electrocoagulation (EC) using magnesium electrodes as anode and stainless steel electrodes as cathode. Several operating parameters on the removal efficiency of boron were investigated, such as initial pH, current density, initial boron ion concentration, NaCl concentration, spacing between electrodes, electrode material, and presence of carbonate concentration. The optimum removal efficiency of 91. 5 % was achieved at a current density of 3 mA/cm² and  pH = 7 using (Mg/St. St. ) electrodes, within 45 min of operating time. The concentration of NaCl was o. 1 g/l with a 0.5cm spacing between the electrodes. First and second order rate equation were applied to study adsorp

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Publication Date
Thu Dec 01 2011
Journal Name
Iraqi Journal Of Physics
vStudy of Linear Shrinkage for Siliceous Materials to Meet Insulating Requirements
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Iraqi siliceous rocks were chosen to be used as raw materials in this study which is concern with the linear shrinkage and their related parameters. They are porcelinite from Safra area (western desert) and Kaolin Duekla, their powders were mixed in certain percentage, to shape compacts and sintered. The study followed with thermal and chemical treatments, which are calcination and acid washing. The effects on final compact properties such as linear shrinkage were studied. Linear shrinkage was calculated for sintered compacts to study the effects of calcination processes, chemical washing, weight percentage, sintering processes, loading moment were studied on this property where the compacts for groups is insulating materials.
Linear

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Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
For Sake of The Economic Reform - With some indication for Iraq
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The imbalances and economic problems which it face the countries, it is a result of international economic developments or changes or global crises such as deterioration in trade, sharp changes in oil prices, increasing global indebtedness, sharp changes in foreign exchange rates and other changes, all that, they affect the economic features of any country. and These influences vary from one country to another according to the rigidity of its economy and its potential in maneuvering with economic plans and actions that would reduce the impact or avoidance with minimal damage. Therefore, the countries  that  suffer from accumulated economic problems as a result of mismanagement and poor planning or suffe

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Publication Date
Thu Jan 30 2020
Journal Name
Journal Of Engineering
Removal of Reactive Dyes by Electro Coagulation Process from Aqueous Solution
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The presence of dyes in wastewater has become a major issue all over the world. The discharge of dyes in the environment is concerned for both toxicological and esthetical reasons. In this study, the removal of dyes from aqueous solution by electrocoagulation using aluminum electrodes as cathode and anode were investigated with the electrocoagulation cell of 1litter. The study included: the impact of various operating parameters on the dyes removal efficiency like pH, NaCl concentration, distance between electrodes, voltage, initial dyes concentration and type of electrodes. The dye (congo red) concentrations were (50, 100, 150, and 200 ppm), stirring speed was 120 rpm at room temperature. pH used was maintained constant

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Publication Date
Sat Oct 01 2022
Journal Name
Al–bahith Al–a'alami
PRESS COVERAGE OF CRISES: (A Research Drawn from a Doctoral Thesis)
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Media is one of the main and effective factors; and it is a tool of crisis management equipment. Media is one of the most dangerous, effective and decisive weapons in modern conflicts; a tool for making events and influencing their events and trends as a means of reporting as the enormous capabilities of media which help media to move very quickly, and cross borders; and overcome obstacles, through many means of audio, reading and visual. As its ability, moreover, to influence the psychological and intellectual control of communities, and behaviors.

Intelligent media is, then, used in crises management and coverage. Crises have been existed with the presence of man on Earth. Thei

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Publication Date
Thu Jul 01 2021
Journal Name
Journal Of Applied Sciences And Nanotechnology
Homogeneity of Lithium Metasilicate-Copper Oxide Glass-Ceramics by Weibull Modulus
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Publication Date
Fri Feb 08 2019
Journal Name
Iraqi Journal Of Laser
Excision of Soft Tissue Oral Lesions by 810 nm Diode Laser
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The present study was conducted on 20 patients suffering from different types of lesion like
pyogenic granuloma, peripheral giant cell granuloma, mucoceles, pregnancy tumour, Fordyce's granules
and irritating fibroma.The cases were selected from outpatient clinic of the Al Kydhemya Teaching
Hospital. Patients were treated by diode laser (810±20 nm) at the affected areas of the oral cavity with
continuous contact focused mode until excision of the lesion with coagulation of the oozing area after
excision. Patients were followed up after 2 days, 7 days and 2 weeks to assess healing process and any
post operative complication. Some of undiagnosed lesion sent for histopathological examination. No
serious complications w

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