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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 15 2026
Journal Name
Biomedicines
EEG-ChTABNet: A Dual-Branch Channel-Wise Transformer with Gated Attention-Branch Network for EEG-Based Classification of Dementia
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Background/Objectives: Early and accurate discrimination of neurological conditions, dementia, stroke and healthy aging, remains a critical clinical challenge. Electroencephalography (EEG) is a non-invasive measure of brain dynamics and entropy-based features obtained from multichannel EEG have shown strong discriminative ability. However, existing deep learning approaches do not sufficiently address the combined challenges of small clinical cohorts and high-dimensional entropy feature spaces. In this study, a novel architecture is proposed for multi-class neurological EEG classification under extreme small-sample conditions. Methods: A novel dual-branch Channel-wise Transformer and Attention-Branch Network (EEG-ChTABNet) are pr to

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Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Statistical quality control charts for measuring educational service quality at Albaha University, Saudi Arabia, from the viewpoint of students
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تم استخدام خرائط ضبط الجودة الإحصائية لتقييم جودة الخدمة التعليمية في جامعة الباحة،  ويهدف هذا البحث إلى استخدام خرائط ضبط الجودة الإحصائية لقياس مستوى الجودة وفجوة الجودة بين توقعات الطلبة وإدراكاتهم لمستوى الخدمة الذي تقدمه جامعة الباحة. حيث تم اختيار عينة من 200 طالب وطالبة عشوائيا باستخدام العشوائية العنقودية من 4 كليات خلال الفترة 01 – 30/2015م، وجمعت البيانات من خلال استبيان جودة الخدمة الذي يقيس ت

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Publication Date
Mon May 27 2019
Journal Name
Al-academy
A Hypothesis of Architectural Environment Exercise for Actor Training (Continuous exercise space workshop – A model): هيثم عبد الرزاق علي
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The peculiarity of the theater does not lie in its dramatic content because many literary genres and other artistic styles share with it in this content. The peculiarity of the theater lies in contemplating the drama through what is architectural, and this architectural axis is what distinguishes its character. It is a spatial poetry which is composed by the laws of physics and chemistry, (Weight, height, distance, rhythm, gravity, impulses and chemical excretions). i.e., what cannot be expressed in words. This is a game of space to exchange and organize energy and communicate in space by the living body, which contains the possibilities of the living drawing in space: in the time and place. This research deals with the importance of the

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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Improvement the bearing capacity of the soil which is supporting the shallow foundation by using bored short micro-piles
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In this paper , concrete micro-piles were used to improve the bearing capacity of the soil which is supporting the shallow foundation by using groups of (4; 6 and 9)bored short micro-piles which have, (D=0.125m and D=0.1m), and length to diameter ratio (L/D) equal to (6; 10 and 12) respectively. To calculate the bearing capacity of the micro-piles,(Tomlinson) and (Lamda) methods were used; also the soil properties were taken from Al-Muthana airport,(Al-Qyssi,2001) [1]. The results show that; increasing the number of piles and/ or the diameters and lengths; and the interaction between the bearing capacity of the shallow foundation with the bearing capacity of the pile group which leads to increasing the strength against the external loads

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Publication Date
Wed Nov 23 2022
Journal Name
Dental Hypotheses
Remineralization of Dentine Caries Using Moringa Oleifera Based Nano-Silver Fluoride: A Single-Blinded, Randomized, Active-Controlled Clinical Trial
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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Kinetic studies of AST isoenzymes I,II,III,IV partially purified from patient,s urine with chroinc renal failure
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In this research, the kinetic studies of four isoenzymes of Asprtate aminotransferase, which partially purified from the urine of chronic renal failure patients were carried out .The four isoenzymes were obeyed Michaelis-Menton's equation and the optimum concentration of their substrate (Aspartic acid) was (166.5x10-3) mole/liter,and their Km values were determined. Four isoenzymesI,II,III,IV have shown an optimum pH at 7.4.The four isoenzymes obeyed Arrhenius equation up to 37º C and their Ea and Q10 constants were determined .

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Publication Date
Wed Oct 31 2018
Journal Name
International Journal Of Research In Pharmaceutical Sciences
The impact of systemic hypertension-related heart remodeling on right ventricle mechanics: A two-dimensional echocardiographic speckle tracking study
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Publication Date
Mon Mar 11 2019
Journal Name
Baghdad Science Journal
The Al-Abiadh Valley Drainage Basin Environmental Aspects Extraction Using Quantitatively Morphometric Analyses of Shuttle Radar Topographic Mission Data
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         The accurate extracting, studying, and analyzing of drainage basin morphometric aspects is important for the accurate determination of environmental factors that formed them, such as climate, tectonic activity, region lithology, and land covering vegetation.

This work was divided into three stages; the 1st stage was delineation of the Al-Abiadh basin borders using a new approach that depends on three-dimensional modeling of the studied region and a drainage network pattern extraction using (Shuttle Radar Topographic Mission) data, the 2nd was the classification of the Al-Abiadh basin streams according to their shape and widenings, and the 3rd was ex

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Publication Date
Wed Feb 01 2023
Journal Name
Measurement: Sensors
Dynamic monitoring of saturated stiff clay soil foundation structure by falling weight deflectometer system under impact loads sensors effect
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Experiments research is done to determine how saturated stiff clayey soil responds to a single impulsive load. Models made of saturated, stiff clay were investigated. To supply the single pulse energy, various falling weights from various heights were tested using the falling weight deflectometer (FWD). Dynamic effects can range from the major failure of a sensitive sensor or system to the apparent destruction of structures. This study examines the response of saturated stiff clay soil to a single impulsive load (vertical displacement at the soil surface below and beside the bearing plates). Such reactions consist of displacements, velocities, and accelerations caused by the impact occurring at the surface depth induced by the impact loads

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Publication Date
Thu Feb 06 2020
Journal Name
Scientific Reports
Waste foundry sand/MgFe-layered double hydroxides composite material for efficient removal of Congo red dye from aqueous solution
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Abstract<p>We aimed to obtain magnesium/iron (Mg/Fe)-layered double hydroxides (LDHs) nanoparticles-immobilized on waste foundry sand-a byproduct of the metal casting industry. XRD and FT-IR tests were applied to characterize the prepared sorbent. The results revealed that a new peak reflected LDHs nanoparticles. In addition, SEM-EDS mapping confirmed that the coating process was appropriate. Sorption tests for the interaction of this sorbent with an aqueous solution contaminated with Congo red dye revealed the efficacy of this material where the maximum adsorption capacity reached approximately 9127.08 mg/g. The pseudo-first-order and pseudo-second-order kinetic models helped to describe the sorption measure</p> ... Show More
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