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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
Tue May 01 2018
Journal Name
Chemical Engineering And Processing - Process Intensification
Studies of mass transfer at a spiral-wound woven wire mesh rotating cylinder electrode
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Mass transfer has been studied at rotating cylinder electrodes fabricated with spiral-wound woven-wire meshes using reduction of copper as a test reaction. The experimental data were correlated by an empirical expression between the Sherwood number and the Reynolds number, both regarding the hydraulic diameter as a characteristic length. It was found that the Sherwood number was dependent upon the Reynolds number to the power of 0.521. An enhancement factor was adopted to compare the efficiency of the new rotating cylinder electrode with previous three-dimensional rotating cylinder electrodes. The results showed that the new type has a mass-transfer enhancement factor 2.3 times higher than those obtained with smooth rotating cylinder electr

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Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
Adsorption of the Color Pollutant onto NiO Nanoparticles Prepared by a New Green Method
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Green synthesis methods have emerged as favorable techniques for the synthesis of nano-oxides due to their simplicity, cost-effectiveness, eco-friendliness, and non-toxicity. In this study, Nickel oxide nanoparticles (NiO-NPs) were synthesized using the aqueous extract of Laurus nobilis leaves as a natural capping agent. The synthesized NiO-NPs were employed as an adsorbent for the removal of Biebrich Scarlet (BS) dye from aqueous solution using adsorption technique. Comprehensive characterization of NiO-NPs was performed using various techniques such as atomic force microscopy (AFM), Fourier transform infrared (FTIR), X-ray diffraction (XRD), Brunauer-Emmett and Teller (BET) analysis, and scanning electron microscopy (SEM). Additionally, o

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Publication Date
Mon Jun 15 2020
Journal Name
Al-academy
Saudi society’s trends towards visiting museums and art galleries: منال بنت مرشد الحربي -حنان بنت يوسف الأحمد-مها بنت عبد الله السنان
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The aim of the research is to identify the trends of Saudi society towards visiting art galleries and museums in light of economic and social transformations after the implementation of the 2030 vision plans. The importance of the research is to track the reasons behind the reluctance of members of society to visit such cultural institutions, and to plan proposals and recommendations for how to attract members of society and motivate them. This research followed the descriptive approach, and the study sample reached 103 members of the Saudi community. several research tools were used in this research such as questionnaire, personal interviews in addition to the researcher notes. The results concluded that the art galleries attract the ap

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Publication Date
Tue Jun 01 2021
Journal Name
Journal Of The College Of Languages (jcl)
The methods used to translate medical terms between Arabic and Spanish: Los métodos utilizados para traducir términos médicos entre árabe y español
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         The present paper deals with medical terms translation and its relationship with the medical text of Arabic and Spanish. Medical translation is the process of transferring texts related to the field of health and medicine to achieve an accurate effective translation from the source language text to the equivalent target language text. The most prominent medical translations are from English to Arabic as most of the syllabuses in Arab countries are taught in English.

       Translation is an innovative work intended to render the original text in the source language into the target language with the highest level of linguistic and intellec

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Publication Date
Fri Sep 02 2022
Journal Name
Rawal Medical Journal
Comminuted intra-articular distal radius fractures treated by ligamentotaxis external fixation with and without bone marrow injection to prevent late metaphyseal collapse
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Objective: To compare the radiological and functional outcomes of patients of Comminuted intraarticular distal radius fractures treated with or without bone marrow injection along with external fixator ligamentotaxis. Methodology: This prospective comparative study on 41 patients with comminuted intra-articular lower end radius fractures distributed patients randomly into two groups depending on whether an aspirate of bone marrow was injected at the fracture site two weeks after fracture management with external fixation ligamentotaxis. Results: The mean age was 35.8 years, with male predominance. The radiological parameters (radial height, radial inclination, and volar tilt) at the 6th month follow up were lower in the group who did not re

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Scopus
Publication Date
Wed Oct 09 2019
Journal Name
International Journal Of Drug Delivery Technology
The comparative study among the MRSAcin, Nisin A and vancomycin, on biofilm formation by Methicillin resistance Staphylococcus aureus isolated from food sources.
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Biofilms formation by pathogens microbial Control considered important in medical research because it is the hazarded virulence factor leading to becoming difficult to treat because of its high resistance to antimicrobials. Glycopeptide antibiotic a (Vancomycin) and the commercial bacteriocin (Nisin A) were used to comparative with purification bacteriocin (MRSAcin) against MRSA biofilm. One hundred food samples were collected from Baghdad markets from July 2016 to September 2016, including (cheese, yogurt, raw milk, fried meat, grilled meat, and beef burger). All samples were cultures; S. aureus was confirmation by macroscopic culture and microscopic examination, in addition to biochemical tests. Methicillin resistance S. asureus (

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Publication Date
Sat Jun 30 2018
Journal Name
College Of Islamic Sciences
Biography Judge Faqih Abu Bakr al-Ansari and its impact on the notation Hadiths (36 AH - 120 AH / 657 AD - 738 AD)
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Followers and their followers (may Allah be pleased with them all) followed the approach of the guidance and the Sunnah of the Messenger of Allah Muhammad (peace be upon him) in the collection and codification of the hadith of the Prophet Muhammad in various Arab and Islamic areas. Subsequent judge Faqih Abu Bakr al-Ansari had a distinct effect during that time immortalized in the pages of our Islamic history in preserving the Sunnah of our great Prophet Muhammad (PBUH) and documenting the constants of Sharia and Islamic jurisprudence and its importance in the activity of intellectual and scientific movement in the Arab Islamic State.

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Publication Date
Sat Jun 10 2017
Journal Name
International Journal Of Current Microbiology And Applied Sciences
A Comparison between Tilapia zilli (Gervais, 1748) (Preciformes: Cichlidae) and Common Carp Cyprinus carpio (Linnaeus, 1758) (Cypriniformes: Cyprinidae) by Staining Bone Technique
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Publication Date
Mon Sep 23 2024
Journal Name
European Journal Of Orthodontics
Poly-Ether-Ether-Ketone versus dead-soft coaxial bonded retainers: a randomized clinical trial. Part 2: periodontal health and microbial biofilm assessment
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Abstract<sec> <title>Background

Retainers have the potential to detrimentally impact periodontal health and contribute to tooth decay.

Objectives

To investigate periodontal health and bacterial biofilm related to Poly-Ether-Ether-Ketone (PEEK) fixed retainers as compared to Dead-soft coaxial fixed retainer (DSC).

Trial design

A two-arm parallel groups single-centre randomized c

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Publication Date
Wed Mar 01 2023
Journal Name
Journal Of Photochemistry And Photobiology A: Chemistry
Multipurpose properties the Z-scheme dimanganese copper oxide/cadmium sulfide nanocomposites for photo- or photoelectro-catalytic, antibacterial applications, and thiamine detection process
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