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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 Dec 11 2006
Journal Name
Iraqi Journal Of Laser
Treatment of Bilateral Vocal Cord Paralysis by 810 nm Diode Laser
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This is prospective study began in Jan. 2003 and concluded in April 2004, was undertaken to examine the benefits of 810 nm diode laser in treatment of four patient with bilateral vocal cord paralysis also to compare the results with conventional treatment Material and methods: 810 nm diode laser 15 watts was used in these cases under general anesthesia, and induction of anesthetic drug done through tracheostomy tube in all patients. All patients were decanulated “Tracheostomy tube removed”, the voice of all preserved within normal. Laser surgery in this case has more benefit and advantage than conventional methods even if the patient need more than on session of laser operation because of high success rate, less complication and easy

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Publication Date
Wed Jun 29 2022
Journal Name
College Of Islamic Sciences
From the flags of The Koofic Grammar: Abdullah Al-Tuaal (243A.H)
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    This research has tackled a scientific figure belongs to Koofi grammatical school. He is Abdullah Al-Tuaal who has occupied the fourth layer among the Koofi grammarians. There was a confusion between him and another Koofi grammarian from the same layer (Mohammed Bin Qaadim) in some old references. This research has clarified this confusion to affirm that they are two different grammarians.This research also tackles the scientific status of Al-Tuaal and the grammatical views that have been ascribed to him in addition to the analysis and discussion of these views. All this in the light of what has been mentioned in grammar books about the issues in which these views were stated.

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Publication Date
Fri Mar 31 2017
Journal Name
Journal Of Engineering
Aerodynamic Characteristics of a Rectangular Wing Using Non-LinearVortex Ring Method
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The aerodynamic characteristics of general three-dimensional rectangular wings are considered using non-linear interaction between two-dimensional viscous-inviscid panel method and vortex ring method. The potential flow of a two-dimensional airfoil by the pioneering Hess & Smith method was used with viscous laminar, transition and turbulent boundary layer to solve flow about complex configuration of airfoils including stalling effect. Viterna method was used to extend the aerodynamic characteristics of the specified airfoil to high angles of attacks. A modified vortex ring method was used to find the circulation values along span wise direction of the wing and then interacted with sectional circulation obtained by Kutta-Joukowsky the

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Publication Date
Tue Dec 11 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Detection of Hypertension among Cardiac Diseases Inpatients at Kirkuk City Hospitals
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Objectives of the study: The main objective of the study is to assess the prevalence of hypertension among
cardiac diseases patients and to fiend out relation ship between hypertension and cardiovascular diseases.
Methodology: A descriptive study, using interviewer and questionnaire technique was conducted on cardiac
diseases inpatients of clinic unite at Kirkuk and Azady hospitals from 17th ,June ,2012 to 1st, March , 2013.
Non – probability (purposive) sample of (148) adult patients, (81) females and (67) males with heart disease are
selected from inpatients of clinic unite at Kirkuk and Azady hospitals at kirkuk city. Questionnaire was
developed to assess the items which are related to heart disease patient's (Dise

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Publication Date
Tue Mar 30 2010
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Numerical study of the mixed convection flow over a square cylinder
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In this work, a numerical study is performed to predict the solution of two – dimensional, steady and laminar mixed convection flow over a square cylinder placed symmetrically in a vertical parallel plate. A finite difference method is employed to solve the governing differential equations, continuity, momentum, and energy equation balances. The solution is obtained for stream function, vorticity and temperature as dependent variables by iterative technique known as successive over relaxation. The flow and temperature patterns are obtained for Reynolds number and Grashof number at (Re= -50,50,100,-100) (positive or negative value refers to aidding or opposing buoyancy , +1 assisting flow, -1 opposing flow) and (102 to 105) , respective

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Publication Date
Tue Jan 08 2019
Journal Name
Iraqi Journal Of Physics
Enhancement of vanadium oxide doped Eu+3 for gas sensor application
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Thin films of vanadium oxide nanoparticles doped with different concentrations of europium oxide (2, 4, 6, and 8) wt % are deposited on glass and Si substrates with orientation (111) utilizing by pulsed laser deposition technique using Nd:YAG laser that has a wavelength of 1064 nm, average frequency of 6 Hz and pulse duration of 10 ns. The films were annealed in air at 300 °C for two hours, then the structural, morphological and optical properties are characterized using x-ray diffraction (XRD), Field emission scanning electron microscopy (FESEM) and UV-Vis spectroscopy respectively. The X-ray diffraction results of V2O5:Eu2O3 exhibit that the film has apolycrystalline monoclinic V2O5 and triclinic V4O7 phases. The FESEM image shows a h

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Publication Date
Thu Sep 01 2016
Journal Name
Journal Of Engineering
Response of Laced Reinforced Concrete One Way Slab to Repeated Loading
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Test results of nine reinforced concrete one way slab with and without lacing reinforcement are reported. The tests were designed to study the effect of the lacing reinforcement on the flexural response of one way slabs. The test parameters were considered is the lacing steel ratios of (0, 0.0025, 0.0045, and 0.0065), flexural steel ratios of (0.0025, 0.0045, and 0.0065) and span to the effective depth ratios of (11, 13, and 16). Two specimens had no lacing reinforcement and the remaining seven specimens had the lacing reinforcement. Four point bending test were carried out, one of the specimens was tested under the static load applied gradually up to failure and the other specimens were tested under repeated load (5 cyc

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Publication Date
Wed May 18 2016
Journal Name
Al-academy
Aesthetic dimension to the formation of postmodern: إيهاب احمد عبد الرضا
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Find taught dimension aesthetic in the formation of post-modernism, which is one of the themes of aesthetics in the stream of postmodernism, is problematic because of the lack of provisions and fixed values reinforce the concept of beauty, and put done technical plastic in the circle of evaluation and judgment aesthetic, this research as an attempt to reveal the aesthetic concepts that can be drawn from artistic experiments in the formation of post-modernism, through the development of those concepts viable mainstream.
Search contains four chapters: the first chapter includes a general approach to the research, has been showcasing the research problem and the importance of research and goal of Search: detection dimension aesthetic in

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Publication Date
Tue Sep 11 2018
Journal Name
Iraqi Journal Of Physics
Gas sensing performance of Sol-gel grown NiO-doped Cr2O3 nanoparticles
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The sensors based on Nickel oxide doped chromic oxide (NiO: Cr2O3) nanoparticals were fabricated using thick-film screen printing of sol-gel grown powders. The structural, morphological investigations were carried out using XRD, AFM, and FESEM. Furthermore, the gas responsivity were evaluated towards the NH3 and NO2 gas. The NiO0.10: Cr2O3 nanoparticles exhibited excellent response of 95 % at 100oC and better selectivity towards NH3 with low response and recovery time as compared to pure Cr2O3 and can stand as reliable sensor element for NH3 sensor related applications.

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Publication Date
Wed Mar 30 2016
Journal Name
College Of Islamic Sciences
The provisions of taking the mother's fare breastfeeding comparative jurisprudential study
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This study aimed to clarify the provisions of taking the mother for breastfeeding in Islamic jurisprudence, a comparative study between doctrines of jurisprudence. The ruling on forcing the mother to breastfeed, and the ruling on taking the mother for breastfeeding while she is in the infallibility of her husband, as well as in several reactionary divorces, and the ruling on breastfeeding in several divorced divorces. On breastfeeding in infallibility Face, as well as a several divorce reactionary, and worth the fare which is in several final divorces, and after the end of the marital relationship, has been proposed a number of recommendations, including it, is recommended to teach the provisions of the mother taking the taxi on breastfe

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