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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 Feb 01 2021
Journal Name
Engenharia Agrícola
HYPERSPECTRAL SPECTROSCOPY TO DETECT DIFFERENT RESPONSES OF TWO SOYBEAN (GLYCINE MAX) CULTIVARS TO CHARCOAL ROT (MACROPHOMINA PHASEOLINA) TOXIN
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Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
The Influence of Biologically Synthesized Copper Nanoparticles on the Biofilm Produced by Staphylococcus haemolyticus 1solated from Seminal Fluid
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     Staphylococcus haemolyticus is one of the most frequently isolated coagulase-negative staphylococci. The ability to form biofilm is considered as one of the most important virulence factors of coagulase negative staphylococci. There is only limited knowledge of the nature of S. haemolyticus biofilms. This study was aimed at evaluating the ability of S. haemolyticus strains to produce biofilm in the presence of copper oxide nanoparticles (CuONPs). The biological synthesis of nanoparticles is an environmentally friendly approach for large-scale production of nanoparticles. Copper oxide nanoparticles were produced in the current study from the S. haemolyticus viable cell filtrate. UV-visible (UV-Vis) spectroscopy, X-ray diffra

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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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Publication Date
Tue Dec 11 2018
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Contribution of Some Managerial Accounting Techniques to Achieve Market Share Requirements / Applied researchin the Al-Muthanna Cement Company
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The research aims to achieve market share requirements and reach the targeted competitive price through the application of management accounting techniques represented by continuous improvement technique and target costing under an Activity Based Cost (ABC) system and Activity Based Management (ABM), In Muthanna Cement Company to reach the rationalization of the cost of the product and maintain the required quality and improve the profitability of the company.

The problem of research has emerged in the inability of local firms to enter into effective competition with other companies operating in the same economic sector, Because of the high cost of its products, Which led to the sale of the product at prices below its cost, and t

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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 Jul 01 2015
Journal Name
Journal Of Educational And Psychological Researches
The impact of education differentiated strategy to modify the alternative conceptions Geographical concepts when students First grade average
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The aim of this study was to know ( the impact of education differentiated strategy to modify the alternative developments of geographical concepts when students first grade average) .
      To achieve the goal of this study , researcher relied on the experimental design of a partial set , the design is ( the experimental group with a control group of post-test )
.

                                              &nbs

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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
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
Sat Oct 01 2011
Journal Name
Journal Of Engineering
THE EFFECT OF SPACE VOLUME ON FREE CONVECTION HEAT TRANSFER FOR ONGITUDINAL FINNED CYLINDER WITH DIFFERENT SLOPE NGLES
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This study deals with free convection heat transfer for the outer surface of two
cylinders of the shape of (Triangular & Rectangular fined cylinders with 8-fins),
putted into two different spaces; small one with dimension of (Length=1.2m,
height=1m, width=0.9m) and large one with dimension of (Length=3.6m, height =3m,
width=2.7m). The experimental work was conducted with air as a heat transport
medium. These cylinders were fixed at different slope angles (0o, 30o, 60o and 90o)
.The heat fluxes were (279, 1012, 1958, 3005, 4419) W/m2, where heat transferred by
convection and radiation. In large space, the results show that the heat transfer from
the triangular finned cylinder is maximum at a slope angle equals

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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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