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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
Sun Aug 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
The impact of service promotion on achieving leadership for business organizations
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The research problem lies in the fundamental questions that revolve around the role of each of the tools of promotion, namely advertising, personal sale, public relations, sales promotion, and direct marketing in achieving leadership for business organizations. Research to know the role of promoting the service in the researched company and whether the promotion of the service is qualified to lead the researched company to leadership, and for this purpose formulated research hypotheses of three hypotheses, the first hypothesis says that there is a significant impact relationship between promotion and entrepreneurship. The second hypothesis aimed to determine the role played by promotion in the researched company to achieve unique

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Publication Date
Tue Feb 01 2022
Journal Name
Methods And Objects Of Chemical Analysis
Spectrophotometric Analysis of Quaternary Drug Mixtures using Artificial Neural network model
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Novel artificial neural network (ANN) model was constructed for calibration of a multivariate model for simultaneously quantitative analysis of the quaternary mixture composed of carbamazepine, carvedilol, diazepam, and furosemide. An eighty-four mixing formula where prepared and analyzed spectrophotometrically. Each analyte was formulated in six samples at different concentrations thus twentyfour samples for the four analytes were tested. A neural network of 10 hidden neurons was capable to fit data 100%. The suggested model can be applied for the quantitative chemical analysis for the proposed quaternary mixture.

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Publication Date
Thu Sep 03 2009
Journal Name
Engineering And Technology Journal
Study on the properties of composite materials produced by centrifugal casting
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سمير خلف فياض * و محسن طالب د.نوال عزت عبد اللطيف*, مجلة الهندسة والتكنولوجيا, 2010

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Publication Date
Fri Aug 20 2021
Journal Name
Iraqi Journal Of Laser
Pulsed Er,Cr:YSGG Laser For Surface Modification of Dental Zerconia Ceramic
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Background: Surface treatment of machined dental zirconia for enhancement of the adhesion to resin cement, using Er,Cr:YSGG  Laser. Materials and Methods: Total number of 42 zirconia disc specimens (9 mm diameter, and 2 mm height) was sintered according to the manufacturer instruction. They are divided into six groups, each group of seven samples. Laser groups (Experiment parameters) were depend on laser total irradiation time, pulse duration, and power. Group (A): 20 sec., 60 µs pulse duration. Group (B): 30 sec., 60 µs pulse duration. Group (C): 40 sec., 60 µs pulse duration. Group (D): 20 sec., 700 µs pulse duration. Group (E): 30 sec., 700 µs pulse duration, with different powers used (1, 1

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Publication Date
Sun Sep 01 2019
Journal Name
Al-khwarizmi Engineering Journal
Adsorption of Heavy Metals from Aqueous Solution onto Sawdust Activated Carbon
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In this study, sawdust as a cheap method and abundant raw material was utilized to produce active carbon (SDAC). Physiochemical activation was utilized where potassium hydroxide   used as a chemical activating agent and carbon dioxide was used as a physical activating agent. Taguchi method of experimental design was used to find the optimum conditions of SDAC production. The produced SDAC was characterized using SEM to investigate surface morphology and BET to estimate the specific surface area. SDAC was used in aqueous lead ions adsorption. Adsorption process was modeled statistically and represented by an empirical model. The highest specific surface area of SDAC was 688.3 m2/gm. Langmuir and Freundlich isotherms were used to

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Publication Date
Sun Dec 01 2013
Journal Name
Baghdad Science Journal
Study the Effect of Solar Radiation Pressure at Several Satellite Orbits
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The effects of solar radiation pressure at several satellite (near Earth orbit satellite, low Earth orbit satellite, medium Earth orbit satellite and high Earth orbit satellite ) have been investigated. Computer simulation of the equation of motion with perturbations using step-by-step integration (Cowell's method) designed by matlab a 7.4 where using Jacobian matrix method to increase the accuracy of result.

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Publication Date
Sat Sep 20 2025
Journal Name
مجلة آداب المستنصرية
Translating the Syntactic Features of Legal Texts from English into Arabic
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This paper examines some syntactic features of English legal texts, and the changes that may be reflected on these features when they are translated into Arabic. For example, passivization, nominalization, complex sentences and modality. The researcher tries to demonstrate why it is difficult to suggest a specific translation of each syntactic feature, especially the modal verbs. The researcher also attempts to provide translations for some legal sentences written in some charters and international organizations. The descriptive methodology is used to identify the characteristics of these syntactic features in order to provide a proper translation of each legal sentence. It has been concluded that the translator has to be aware of the preci

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Publication Date
Mon Dec 23 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Use of Human Umbilical Cord Serum to Treat Animal Skin Burns
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Objective: The objective of the study was to test the hypothesis, that umbilical cord blood crude serum applied topically with its high concentration of growth factors may promote an early healing for animal models with burn injury.

Methods:  Fresh human umbilical cord blood UCBS was collected and screened for transmitted diseases such as hepatitis B, hepatitis C and HIV. Mice and rabbits were scalded by boiling water and chemical burning by NaOH, then treated with UCBS. In comparison with a Cetrimide treated group and a control group (without treatment). The UCBS was subjected to microbial testing to demonstrate the presence or absence of extraneous viable contaminating microorganisms.

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Solvability of Some Types for Multi-fractional Integro-Partial Differential Equation
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In this article, the solvability of some proposal types of the multi-fractional integro-partial differential system has been discussed in details by using the concept of abstract Cauchy problem and certain semigroup operators and some necessary and sufficient conditions. 

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Publication Date
Thu Jun 10 2010
Journal Name
Iraqi Journal Of Laser
Improvement of Nonlinear Optical Properties for Mixture Laser Dyes Doped PMMA
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The spectral characteristics and the nonlinear optical properties of the mixed donor (C-480) acceptor (Rh-6G) have been determined. The spectral characteristics are studied by recording their absorption and fluorescence spectra. The nonlinear optical properties were measured by z-scan technique, using Q-switched Nd: YAG laser with 1064 nm wavelength. The results showed that the optimum concentration of acceptor is responsible for increasing the absorption and the emission bandwidth of donor to full range and to 242 nm respectively by the energy transfer process, also the efficiency of the process was increased by increasing the donor and acceptor concentration. The obtained nonlinear properties results of the mixture C-480/ Rh-6G showed

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