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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
Wed Feb 22 2023
Journal Name
Iraqi Journal Of Science
Test the Cytotoxicity of Pleurotin Extracted from an Edible Mushroom Pleurotus osteratus Against Three Human Carcinoma Cell Line
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The study included selection six species of the fungi related to Pleurotus genus were evaluated for their ability to production of Pleurotin, one of them, Pleurotus ostreatus (P.11) was isolated and identified in the present study. Pleurotin was extracted with screening by Thin Layer Chromatography (TLC) and quantification High Performance Liquid Chromatography (HPLC). Cytotoxicity of Pleurotin extracted from P. ostreatus (P.11) grown in different sugar sources (galactose, mannitol, sucrose, dextrose and lactose) liquid media was test against three selected cancer cell lines, CaSki, MCF-7 and A549 addition to Human Non Cancer Fibroblast Cell Line (MRC-5). Pleurotin of P. ostreatus (P.11) grown in galactose induced the significant highest

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Publication Date
Fri Sep 01 2023
Journal Name
Al-khwarizmi Engineering Journal
Removal of Ciprofloxacin Antibiotic from Synthesized Aqueous Solution Using Three Different Metals Nanoparticles Synthesized Through the Green Method
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This study investigates the possibility of removing ciprofloxacin (CIP) using three types of adsorbent based on green-prepared iron nanoparticles (Fe.NPs), copper nanoparticles (Cu. NPS), and silver nanoparticles (Ag. NPS) from synthesized aqueous solution. They were characterized using different analysis methods. According to the characterization findings, each prepared NPs has the shape of a sphere and with ranges in sizes from of 85, 47, and 32 nanometers and a surface area of 2.1913, 1.6562, and 1.2387 m2/g for Fe.NPs, Cu.NPs and Ag.NPs, respectively. The effects of various parameters such as pH, initial CIP concentration, temperature, NPs dosage, and time on CIP removal were investigated through batch experiments. The res

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Publication Date
Mon Jun 01 2020
Journal Name
Iraqi Journal Of Physics
Effect depositions parameters on the characteristics of Ni0.5Co0.5Fe2O4 nanocomposite films prepared by DC reactive magnetron Co-Sputtering technique
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In this work, spinel ferrites (NiCoFe2O4) were prepared as thin films by dc reactive dual-magnetron co-sputtering technique. Effects of some operation parameters, such as inter-electrode distance, and preparation conditions such as mixing ratio of argon and oxygen in the gas mixture, on the structural and spectroscopic characteristics of the prepared samples were studied. For samples prepared at inter-electrode distance of 5 cm, only one functional group of OH- was observed in the FTIR spectra as all bands belonging to the metal-oxygen vibration were observed. Similarly, the XRD results showed that decreasing the pressure of oxygen in the gas mixture lead to grow more crystal planes in the samples prepare

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Publication Date
Fri Mar 01 2019
Journal Name
Al-khwarizmi Engineering Journal
Design of PV Solar Energy Generator using MPPT Technique to Control Single Input/Multiple Outputs (DC-DC) Converter
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The paper presents the design of a system consisting of a solar panel with Single Input/Multiple Outputs (DC-DC) Buck Converter by using Simulink dialogue box tools in MATLAB software package for simulation the system. Maximum Power Point Tracking (MPPT) technique depending on Perturb and Observe (P&O) algorithm is used to control the output power of the converter and increase the efficiency of the system. The characteristics of the MSX-60 PV module is chosen in design of the system, whereas the electrical characteristics (P-V, I-V and P-I curves) for the module are achieved, that is affected by the solar radiation and temperature variations. The proposed design module has been found to be stable for any change in atmospheric tempera

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Publication Date
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Laser
Hong-Ou-Mandel Dip Measurements of Two Independent Weak Coherent Pulses for Free Space Quantum Key Distribution Systems
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Preparation of identical independent photons is the core of many quantum applications such as entanglement swapping and entangling process. In this work, Hong-Ou-Mandel experiment was performed to evaluate the degree of indistinguishability between independent photons generated from two independent weak coherent sources working at 640 nm. The visibility was 46%, close to the theoretical limit of 50%. The implemented setup can be adopted in quantum key distribution experiments carried out with free space as the channel link, as all the devices and components used are operative in the visible range of the electromagnetic spectrum.

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Publication Date
Wed Aug 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
(( Technology's role Time driver Activity-based costing at Provide of information for economic units for customer profitability analysis ))
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  The economic units always sought to maintain its market position and Trchinh the technology management and modern methods that will support success factors .vdila about it has become a customer and one profitability analysis of the most practical way benefit of economic units as modern management focus their attention on achieving this satisfaction, as the customers make up the axis of the success of every organization and that there are many government units aiming to profit directs attention to customers and the number of these units increased continuously. The administration used the customer profitability analysis in order to obtain information to assist in making and decision-making process. How to use modern tec

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Publication Date
Fri Aug 01 2025
Journal Name
مجلة كلية التربية الاساسية
The Effect of the Cornell Note-Taking Strategy on Systematic Thinking Skills Among Second-Year Intermediate Female Students
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The current research aims to identify the effect of the note-taking strategy (CORNELL) on systematic thinking among second-grade female students in government daytime secondary and intermediate schools. Al-Fadhila School was intentionally chosen to be its student sample for the research affiliated with the First Karkh Directorate for the academic year (2024-2025). Then one of the two sections was randomly chosen to represent the experimental group that studies according to the note-taking strategy (CORNELL) and the other the control group that studies according to the usual method. The equivalence of the two research groups was verified by a set of variables, which were represented by chronological age in months, previous achievement in che

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Publication Date
Mon Jan 01 2024
Journal Name
Infocommunications Journal
On the Performance of Metamaterial based Printed Circuit Antenna for Blood Glucose Level Sensing Applications: A Case Study
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Due to the urgent need to develop technologies for continuous glucose monitoring in diabetes individuals, poten tial research has been applied by invoking the microwave tech niques. Therefore, this work presents a novel technique based on a single port microwave circuit, antenna structure, based on Metamaterial (MTM) transmission line defected patch for sensing the blood glucose level in noninvasive process. For that, the proposed antenna is invoked to measure the blood glu cose through the field leakages penetrated to the human blood through the skin. The proposed sensor is constructed from a closed loop connected to an interdigital capacitor to magnify the electric field fringing at the patch center. The proposed an tenna sensor i

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Publication Date
Thu Dec 24 2020
Journal Name
Advances In Civil Engineering
Analytical study on torsional behavior of concrete beams strengthened with fiber reinforced polymer laminates using softened truss model
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This study aimed at evaluating the torsional capacity of reinforced concrete (RC) beams externally wrapped with fiber reinforced polymer (FRP) materials. An analytical model was described and used as a new computational procedure based on the softened truss model (STM) to predict the torsional behavior of RC beams strengthened with FRP. The proposed analytical model was validated with the existing experimental data for rectangular sections strengthened with FRP materials and considering torque-twist relationship and crack pattern at failure. The confined concrete behavior, in the case of FRP wrapping, was considered in the constitutive laws of concrete in the model. Then, an efficient algorithm was developed in MATLAB environment t

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Publication Date
Sun May 10 2020
Journal Name
Baghdad Science Journal
Temperature Impacts on the Cardiac Activity of the Snail Pomacea canaliculata from Shatt Al-Arab Region, Basrah, Iraq
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The effects of temperature on an exotic aquatic snail Pomacea canaliculata  (Lamarck, 1819) collected from the Shatt Al-Arab intertidal zone were investigated. A series of laboratory experiments were conducted during the summer period of 2017. Individuals of new born snails hatched in the laboratory from adult snails were collected from Shatt Al-Arab intertidal zone, and subjected to five fixed temperatures: 15, 25, 35, 40 and 45 Cº, after short term thermal acclimation. The heartbeats (HB) were counted at each temperature level. The results showed significant  direct increase of HB from 15 Cº (19.8 HB/min) up to 25 Cº (76 HB/min) (P<0.05)  as well as from 25 Cº to 35 Cº (93 HB/min). At 40 Cº the snail HB

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