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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
Thu Feb 06 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Efficacy of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint
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Background: Temporomandibular joint disorders refer to a group of heterogeneous pain and dysfunction conditions involving the masticatory system, reducing life quality of the sufferers. Arthrocentesis is simple and less invasive surgical procedure for the treatment of internal derangement than arthroscopy and better than other conservative procedures such as drugs, occlusal appliances and physiotherapy. The aim of the study was to evaluate the effect of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint for the restoration of its function, reducing pain and preventing further deterioration of the temporomandibular joint dysfunction. Materials and methods: This study was perfo

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Publication Date
Thu Feb 07 2019
Journal Name
Iraqi Journal Of Laser
The Effect of 532 nm Diode Pumped Solid State (DPSS) Laser in Combination with Safranin on the Growth of Pseudomonas aeruginosa and Staphylococcus aureus in Vitro
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The effect of 532nm Diode Pumped Solid State (DPSS) laser at power density of 5.234 W/cm2 on the growth of Gram-negative Pseudomonas aeruginosa and Gram-positive Staphylococcus aureus was evaluated. These bacteria were isolated from samples taken from burn and infected wound areas of 55 patients admitted to the burn-wound unit in Al-Kindy teaching hospital in Baghdad during the period from October 2012 to March 2013. Each isolate was identified using microscopic, cultural and biochemical methods. A standard bacterial suspension was prepared for each isolate. Serial dilutions were then prepared and a dilution of 10-5 was selected. Irradiation experiments included four groups: (L-P-) bacterial suspension in saline solution, (L-P+) bacteria

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Publication Date
Tue Dec 22 2020
Journal Name
Lecture Notes In Civil Engineering
Geometric Nonlinear Synthetic Earthquake Analysis of Base Isolated Tall Steel Buildings Under Site-Specific Seismic Loading
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Publication Date
Fri Dec 30 2022
Journal Name
Iraqi Journal Of Science
Electrical Resistivity Imaging (ERI) for Identifying Near-surface Bodies at Diyala University site, NE of Iraq
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      The current research demonstrates the ERI method's effectiveness as a supplementary engineering site investigation approach. Engineering site research is important to indicate the subsoil of proposed production sites. The benefit of the dipole-dipole array for ERI electrical resistivity imaging is that it provides informative records of subsurface geology and condition along with profiles. The dipole-dipole array was performed along with three parallel profiles at the Diyala University site to identify the buried facilities (pipes and cables) in the area. The buried electric cable embedded in a plastic tube was used for simulation to report and verify the field resistivity results. Interpretation of field facts confirmed that

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Publication Date
Mon Feb 04 2019
Journal Name
Iraqi Journal Of Physics
Risks assessment for the retrieval of radioactive waste from the old Russian cemetery Al -Tuwaitha site
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In this work the radioactive wastes in the Old Russian
Cemetery Al -Tuwaitha site were classified according to risks for
workers who are involved in the retrieval process. The exposure
assessment results expressed as estimates of radionuclide intakes by
inhalation and ingestion, exposure rates and duration for external
exposure pathways, and committed effective dose equivalents to
individuals from all relevant radionuclides and pathways. Results
showed the presence of natural radionuclides Ra-226, Th-234 and K-
40, as well as the produced radionuclide Cs-137 and Eu-152 in the
cemetery wells. The absorbed doses from the waste were classified to
two categories; exempt waste and low level waste according to

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Crossref
Publication Date
Sat Apr 15 2023
Journal Name
Iraqi Journal Of Science
Evaluation of the Ground Water in Baghdad Governorate / Iraq
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The coverage area of Baghdad Governorate area is considered as a part of the
Mesopotamia plain, which belongs to the unstable shelf. This area is totally covered
by quaternary sediments. The sediments are composed mainly by cyclic alteration of
clay, silt, sand and very fine gravels. Quaternary sediments represent the main
aquifer for all parts of Baghdad governorate.
Arc GIS 9.3 and GMS 6.5 programs were used in drawing high accurate
estimating maps, to define salinity, type of the ground waters, the general direction
of their movement, the distribution values of transmissivity of upper aquifer, with
distribution and the amount of draw down for these wells, also drawing map for the
ground waters depth zones.

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Publication Date
Fri Dec 14 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Personal Digital Assistant Acceptance in Nursing Education
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Objective:To measure the acceptance level of the Personal Digital Assistance (PDA)’suse among nursing students as a tool of education in the Kingdom of Saudi Arabia. Methodology: Eighty-nine nursing students participated in this cross-sectional descriptive study by completing a questionnaire based on the Technology Acceptance Model (TAM) by Davis. Two dimensions were explored and evaluated; (1) the applicability of the TAM model in assessing this technology; and (2) the overall percentage of students’ agreement on the different TAM variables. Results: This study presented significant positive influence bet

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Publication Date
Thu Apr 20 2023
Journal Name
Maaen Journal For Medical Sciences
Evaluation of heated cure acrylic immersed in ozonated water
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Background: Denture cleansing is an important step that can prevent the spread of infection and improve a patient's health, the durability of the dentures, and the overall quality of life; therefore, it is necessary to choose a suitable cleanser that, in addition to being effective, does not have an unfavorable effect on the qualities of the denture base resin itself when used for an extended period. Aim: This research aims to assess the effects of ozonated water on the surface roughness and hardness of heat-cured acrylic resin by immersion technique. Materials: Sixty bars shapemade of heat-cured acrylicweremanufactured.Thirty samples for every test, including: (surface hardness and surface roughness). Then, these samples were divided into

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Publication Date
Mon Jun 30 2014
Journal Name
Al-kindy College Medical Journal
Evaluation of Serum RANKL Level in Acute Coronary Syndrome
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Background: Acute coronary syndrome (ACS) is a common disease, and a major determinant of morbidity and mortality in all races. The pleiotropic effects of the receptor activator of nuclear factor-kappa B ligand (RANKL) such as modulation of cell survival, mineralization and inflammation, make it an interesting candidate mediator in the progression and destabilization of atherosclerotic lesions.Objectives: This study was performed to investigate the role of RANKL in the pathogenesis of ACS.Methods: The levels of RANKL were measured by ELISA method in sera of 60 ACS patients, 31 patients with unstable angina (UA) and 29 patients with myocardial infarction (MI) in comparison with 20 apparently healthy controls.Results: Current data indicate

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Publication Date
Wed Dec 12 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Youth's Health Risk Behaviors in Baghdad City
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Objective(s): To evaluate youth's health risk behaviors in Baghdad City and to determine the relationship between such behaviors and the youth's demographic characteristics of age, gender and grade. Methodology: A descriptive study, using the evaluation approach, is carried out to evaluate youth's health risk behaviors in Baghdad City for the period of January 26th 2016 to May 20th 2016. A non-probability "purposive" sample of (160) University students is selected for the purpose of the study from four groups of colleges (medical, engineering, sciences, and education) and it is equally distributed of

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