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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 Jun 05 2023
Journal Name
Journal Of Engineering
Compressive Behavior of Fiber Reinforced Concrete Columns Rehabilitated with CFRP Warps
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Over the last few years, there has been a worldwide increase in the use of composite materials for rehabilitation of deficient reinforced concrete structures. One important application of this technology is the use of Carbon Fiber Reinforced Polymer (CFRP) jacket to provide external confinement of reinforced concrete columns. Square concrete column specimens 100×100×1000 mm with concrete
compressive strength of about 30 and 50 MPa, steel fiber volume fraction 0%, 0.5%, 0.75%, and percentage of longitudinal reinforcement 2.01%, 3.14% and 4.52% were tested until failure in previous research. In this research seven tested columns were repaired and rehabilitated using one layer of CFRP flexible wraps and tested to determine their ultim

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Publication Date
Sun Jan 01 2023
Journal Name
International Journal Of Humanities And Social Sciences/ Rimak
AN EMPIRICAL ANALYSIS OF EDUCATIONAL RESEARCH BASED ON CRITICAL DISCOURSE ANALYSIS
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APDBN Rashid, International Journal of Humanities and Social Sciences/ RIMAK, 2023

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Publication Date
Tue Feb 06 2024
Journal Name
Research Square
Bioremediation of Cellulosic Wastes by Using Orthodillo chiltoni (Vandel, 1973), Isopoda
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Terrestrial isopods play an important role in the biodegradation of many wastes which gives agreat importance in the nutrient cycles and ecosystem services , therefore this paper aims to use species Orthodillo chiltoni (Vandel, 1973) as a model organism in bioremediation of urban environment with municipal wastes, agricultural fields, parks and markets wastes. Samples of these wastes included potato peels, orange fruit leaves, thyme plant and sawdust,cardboard residues , the experiments were carried out in laboratory condition similar to the living environment of this species in terms of temperature, humidity and intensity lighting. The applied results have shown that

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Publication Date
Tue Nov 01 2022
Journal Name
Journal Of Engineering
Study The Impact of Geopolymer Mortar Reinforced by Micro Steel Fibers
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In this research, geopolymer mortar had to be designed with 50% to 50% slag and fly ash with and without 1% micro steel fiber at curing temperature of 240℃. The molarity of alkaline solution adjusted with 12 molar sodium hydroxid to sodium silicate was 2 to 1, reaspectivly. The heat of curing increased the geopolymerization proceses of geoplymer mortar, which led to increasing strength, giving the best result and early curing age. The heat was applied for two days by four hours each day. It was discovered in the impact test that the value first crack of each mix was somewhat similar, but the failure increased 72%  for the mixture that did not contain fiber. For the energy observation results it was shown that the mixt

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Publication Date
Sun Nov 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Emissions Investigating of Carbon Dioxide Generated by the Iraqi Cement Industry
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Abstract<p>The most used material in the world after water is concrete, which depends mainly on its manufacture of cement leading to the emission of carbon dioxide (CO<sub>2</sub>), flying dust, and other greenhouse gasses (GHGs) resulting in pollution of the atmosphere. The emission of CO<sub>2</sub> from cement production is approximately 5% of the global anthropogenic CO<sub>2</sub>. This research focuses on investigating the amount of CO<sub>2</sub> emission from the Iraqi General Cement Company plants includes the cement factories of Kirkuk, Al-Qa’em, Fallujah, and Kubaisa, using the GHGs Protocol Measures Program (specifically cement based-method).</p> ... Show More
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Publication Date
Tue Dec 01 2020
Journal Name
Baghdad Science Journal
Detection of Suicidal Ideation on Twitter using Machine Learning & Ensemble Approaches
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Suicidal ideation is one of the most severe mental health issues faced by people all over the world. There are various risk factors involved that can lead to suicide. The most common & critical risk factors among them are depression, anxiety, social isolation and hopelessness. Early detection of these risk factors can help in preventing or reducing the number of suicides. Online social networking platforms like Twitter, Redditt and Facebook are becoming a new way for the people to express themselves freely without worrying about social stigma. This paper presents a methodology and experimentation using social media as a tool to analyse the suicidal ideation in a better way, thus helping in preventing the chances of being the victim o

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Publication Date
Sat Sep 30 2023
Journal Name
Iraqi Journal Of Science
Study on tssC1 Gene Mediating Biofilm Antibiotics Resistance of Pseudomonas aeruginosa
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P. aeruginosa is a famous bacterium that causes several diseases and has a high ability to be a multidrug resistant organism that is linked with the formation of biofilm. This study aimed to investigate tssC1 gene role in the resistance of different antibiotics in the presence of biofilm. We constructed biofilm for the isolates under the study and showed the effect of different antibiotics on biofilm formation and maturation. The presence of the gene was detected through achieving PCR reaction. Finally, tssC1 gene variation was determined through sequencing and aligning the sequencing products. The results showed that most of the isolates (80%) formed biofilm that played a role in the resistance of different antibiotics which could

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Publication Date
Sun Jun 09 2024
Journal Name
2024 Ieee 52nd Photovoltaic Specialist Conference (pvsc)
Exploring the Capacitance-Voltage Response of Metal Halide Perovskite Solar Cells
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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Studying the biological activity of some Antimony Compounds with amino acids
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In this work four complexes of antimony were prepared ,Na[SbO(gly)2],Na[SbO(Asp)2],Na[SbO(Tyrosin)2], Na [SbO(phen alanin)2]. by reaction SbOCl with salts amino acids identifiefid these complexes by FTIR ,their conductivity was measured and also their biological activity against two types of bacteria was studied ,they were biologically active.

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Publication Date
Wed Jan 01 2020
Journal Name
Medical Journal Of Babylon
Impact of chronic hepatitis B virus infection on bone mineral density
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Background: Chronic hepatitis B virus (HBV) infection is a common health problem that has a worldwide distribution. Apart from the direct effect of the virus on the liver, there are many extrahepatic manifestations among which the probable effect on bone turnover associated with low bone mineral density (BMD). Objectives: This study aimed to determine the association between treated and untreated chronic HBV infection with BMD. Methods: This is a cross-sectional study which included a total of 48 patients with chronic HBV (28 patients treated with tenofovir-disoproxil-fumarate [TDF] antiviral drug and 20 patients have not yet started treatment). Other age- and sex-matched 30 apparently healthy individuals were recruited to represent the hea

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