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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
Sun Feb 03 2019
Journal Name
Iraqi Journal Of Physics
Influence of non-thermal argon plasma needle on blood coagulation
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Non-thermal argon plasma needle at atmospheric pressure was
constructed. The experimental setup was based on a simple and low
cost electric component that generates a sufficiently high electric
field at the electrodes to ionize the argon gas which flow at
atmospheric pressure. A high AC power supply was used with 1.1
kV and 19.57 kHz. Non-thermal Argon plasma used on blood
samples to show the ability of non-thermal plasma to promote blood
coagulation. Three tests have been done to show the ability of plasma
to coagulate both normal and anti-coagulant blood. Each blood
sample has been treated for varying time from 20sec. to 180sec. at
different distances. The results of the current study showed that the
co

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Publication Date
Sat Jan 01 2022
Journal Name
Aip Conference Proceedings
Molecular identification of dermatophytes by arbitrarily primed polymerase chain reaction
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Publication Date
Sat Oct 01 2022
Journal Name
The Egyptian Journal Of Hospital Medicine
Developing Gold-Resveratrol Nanoconjugates for Management of Rheumatoid Arthritis (RA)
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
the coincidence lefschetz number for self-maps of lie groups
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Let/. It :0 ---0 G be any two self maps of a compact connected oriented Lie group G. In this paper, for each positive integer k , we associate an integer with fk,hi . We relate this number with Lefschetz coincidence number. We deduce that for any two differentiable maps f, there exists a positive integer k such that k 5.2+1 , and there is a point x C G such that ft (x) = (x) , where A is the rank of G . Introduction Let G be an n-dimensional com -pact connected Lie group with multip-lication p ( .e 44:0 xG--+G such that p ( x , y) = x.y ) and unit e . Let [G, G] be the set of homotopy classes of maps G G . Given two maps f , f G ---• Jollowing [3], we write f. f 'to denote the map G-.Gdefined by 01.11® =A/WO= fiat® ,sea Given a point g

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Publication Date
Thu Apr 01 2021
Journal Name
Pakistan Journal Of Statistics
Estimation intensity radiation of chest X-ray (CXR) with application
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In this research we assumed that the number of emissions by time (𝑡) of radiation particles is distributed poisson distribution with parameter (𝑡), where  < 0 is the intensity of radiation. We conclude that the time of the first emission is distributed exponentially with parameter 𝜃, while the time of the k-th emission (𝑘 = 2,3,4, … . . ) is gamma distributed with parameters (𝑘, 𝜃), we used a real data to show that the Bayes estimator 𝜃 ∗ for 𝜃 is more efficient than 𝜃̂, the maximum likelihood estimator for 𝜃 by using the derived variances of both estimators as a statistical indicator for efficiency

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Scopus
Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Strategic relationship training to promote self-growth of the individual
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The main objective of the research is to identify the role of strategic training and its effect on enhancing the self-growth of the individual. Stratigic training represents a contemporary tendency. that is adopted by business organizations in carrying out their activities and tasks.

It is worth to mention, that self-growth of the individual is one of the indictors used to determine the ability of organization to a achieve its goals. 

The problem of the research has pointed out to the minimum awareness of the important role played by training strategy in enhancing the self-growth of the individual. The researcher has adopted an analytical approach, in collecting and analyses

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Crossref
Publication Date
Sun Jan 02 2011
Journal Name
Education College Journal/al-mustansiriyah
Double Stage Shrinkage Estimators of Two Parameters Generalized Rayleigh Distribution
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Publication Date
Sat Nov 03 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Incidence of Seasonal Diarrhea among Children at Child's Central Hospital
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Objective: Diarrhea is a symptom of a variety of conditions may attack the child. It considered one of
mam causes of mortality rates especially in low socio- economic level countries. The child can be
easily got dehydration and pass from loss of too much body fluid and due to the Common thoueht of
increasing the incidence of diarrhea during summer season, this study is done to find out the relation
between the high incidences rate of diarrhea and weather variation
Methodology: This survey conducted in AL- Markazi Child's Teaching Hospital for the year 2005 the
data were gathered from hospital records for the period (January - December) and age groups
taxonomy used by hospital applied. Descriptive statistical analysis

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Publication Date
Thu Nov 03 2022
Journal Name
International Journal Of Special Education
Adsorption of Methylene Blue from Their Aqueous Solution: Review Article
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Various industrial applications include the dyeing of textiles, paper, leather, and food products, as well as the cosmetics industry. Physic-chemical methods are required to breakdown dyes because they are known to be harmful and persistent in the environment. Many companies' treated effluents contain small amounts of dyes. When it comes to removing dye from wastewater, adsorption has verified to be aneconomical alternative to more traditional treatment procedures. It's important to degrade color impurities in industrial effluents since they constitute a serious health and environmental concern. One way that's been tried is using clay minerals as an adsorbent. Using adsorption for removing

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Publication Date
Wed Nov 07 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of a dietary education program upon hypertensive clients' information
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Objective: To determine the effectiveness of a dietary educational program upon the hypertensive client’s
information.
Methodology: The sample of the study consists of (60) hypertensive clients who attended Al Anbar Health Office –Al
Andalus Health Center during the period of the study from the14th of March 2010 to the 30th of September 2010. The
sample is divided into two groups; study group (30) hypertensive clients who received dietary educational program
and control group (30) hypertensive clients who received a routine care from the center. Three major instruments
were used; these instruments included (1) knowledge test which was applied on both groups pretest and eight weeks
post-test (2) questions to know

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