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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 Sep 02 2021
Journal Name
International Journal Of Drug Delivery Technology
Role of Lactobacillus plantarum and Lactobacillus acidophilus as a Treatment of Cryptosporidiosis in Mice
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Objective: To evaluate the therapeutic activity of probiotics mixture of Lactobacillus plantarum and Lactobacillus acidophilus towards Cryptosporidium infection in experimentally infected mice. Oocysts of Cryptosporidium were separated from the stool of humans to infect mice. Methods: Forty male albino mice were split equally into four groups, every group contained 10 mice, the group I (early treated group), were treated from the 1st day from infection to the 11th post-infection, group II (late treated group), were treated from the 4th day from infection to the 15th post-infection, and group (III) (untreated group), were mice considered as a positive control group. Results: It was showed that daily application of a mixture of L. plantarum w

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Publication Date
Fri Feb 08 2019
Journal Name
Journal Of The College Of Education For Women
THE IMPACT OF MONEY MATTERS ON THE CHARACTERS IN MURIEL SPARK’S NOVEL THE BALLAD OF PECKHAM RYE
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Money matters exert a considerable influence on man’s life-style, social
rank and his relationship with other people. This paper aims at exploring the impact
of money matters on the characters’ inner feelings, social status, and personal
relationships in Muriel Spark’s modern novel The Ballad Of Peckham Rye. This
paper aspires to show that Spark’s subtle portrayal of characters reveals the
dominance of money matters over human and social relationships.
Muriel Spark ( 1918-2006) is a modern Scottish novelist whose wit and
detached sense of humour has brought her prolific body of both popular and critical
acclaim. Spark is interested not in building suspense but in exploring the moral
significance of the

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Publication Date
Tue Feb 14 2017
Journal Name
مجلة كلية التربية للعلوم الصرفة ابن الهيثم
synthesis and characterization of New Bidentate schiff base Ligand Type(NO)Donor Atoms Derived from isatin and 3-Amino benzoic acid and Its complexes with Co(||),Cu(||),Cd(||)and Hg(||)Ions
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synthesis and characterization of New Bidentate schiff base Ligand Type(NO)Donor Atoms Derived from isatin and 3-Amino benzoic acid and Its complexes with Co(||),Cu(||),Cd(||)and Hg(||)Ions

Publication Date
Fri Dec 01 2023
Journal Name
Advances In Science And Technology Research Journal
Experimental Investigation and Fuzzy Based Prediction of Titanium Alloy Performance During Drilling Process
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Publication Date
Wed Sep 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
A Viscoplastic Modeling for Permanent Deformation Prediction of Rubberized and Conventional Mix Asphalt
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Publication Date
Fri Jun 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Correlation for fitting multicomponent vapor-liquid equilibria data and prediction of azeotropic behavior
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Correlation equations for expressing the boiling temperature as direct function of liquid composition have been tested successfully and applied for predicting azeotropic behavior of multicomponent mixtures and the kind of azeotrope (minimum, maximum and saddle type) using modified correlation of Gibbs-Konovalov theorem. Also, the binary and ternary azeotropic point have been detected experimentally using graphical determination on the basis of experimental binary and ternary vapor-liquid equilibrium data.

            In this study, isobaric vapor-liquid equilibrium for two ternary systems: “1-Propanol – Hexane – Benzene” and its binaries “1-Propanol –

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Publication Date
Fri Dec 30 2022
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Artificial Intelligent Models for Detection and Prediction of Lost Circulation Events: A Review
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Lost circulation or losses in drilling fluid is one of the most important problems in the oil and gas industry, and it appeared at the beginning of this industry, which caused many problems during the drilling process, which may lead to closing the well and stopping the drilling process. The drilling muds are relatively expensive, especially the muds that contain oil-based mud or that contain special additives, so it is not economically beneficial to waste and lose these muds. The treatment of drilling fluid losses is also somewhat expensive as a result of the wasted time that it caused, as well as the high cost of materials used in the treatment such as heavy materials, cement, and others. The best way to deal with drilling fluid losses

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Publication Date
Sun Jun 30 2013
Journal Name
Al-khwarizmi Engineering Journal
Efficiency Prediction and Performance Characterization of Photovoltaic Solar Panel at Baghdad Climate Conditions
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The performance of a solar cell under sun radiation is necessary to describe the electrical parameters of the cell. The Prova 200 solar panel analyzer is used for the professional testing of four solar cells at Baghdad climate conditions. Voltage -current characteristics of different area solar cells operated under solar irradiation for testing their quality and determining the optimal operational parameters for maximum electrical output were obtained. A correlation is developed between solar cell efficiency h and the corresponding solar cell parameters; solar irradiance G, maximum power Pmax, and production date P. The average absolute error of the proposed correlation is 5.5% for 40 data points. The results also show th

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Publication Date
Fri May 01 2026
Journal Name
Civil Engineering Journal
Bearing Capacity Enhancement of Hexagonal Skirted Footings: Numerical, Regression, and ANN-Based Prediction
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This paper presents a comprehensive numerical analysis of the improvement in bearing capacity and settlement performance of hexagonal shallow footings with inclined skirts. Various numerical analyses were conducted using PLAXIS 3D to investigate the influence of skirt length-to-footing width (L/B) ratios and skirt inclination angles (θ) on hexagonal footings in loose sand. The models showed very good agreement with experimental data reported in previous studies, with an R² value of 0.996 and a maximum error of less than 4.31%. It was concluded that the inclusion of inclined skirts has a positive effect on bearing capacity, increasing it by up to approximately 2.97 times compared to non-inclined configurations, while significantly

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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Synthesis of Bimetallic Au–Pt / TiO2 Catalysts as an Efficient Catalyst for the Photodegradation of Crystal Violet Dye
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     Bimetallic Au –Pt catalysts supporting TiO2 were synthesised using two methods; sol immobilization and impregnation methods. The prepared catalyst underwent a thermal treatment process at 400◦ C, while the reduction reaction under the same condition was done and the obtained catalysts were identified with transmission electron microscopy (TEM) and energy-dispersive spectroscopy (EDS). It has been found that the prepared catalysts have a dimension around 2.5 nm and the particles have uniform orders leading to high dispersion of platinum molecules .The prepared catalysts have been examined as efficient photocatalysts to degrade the Crystal violet dye under UV-light. The optimum values of Bimetallic Au –Pt catalysts supp

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