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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 Nov 21 2019
Journal Name
Al-kindy College Medical Journal
The The Role of Breast Sonography and Ductography in the Evaluation of Different Causes of the Nipple Discharge
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ABSTRACT

 

Background : The aim of this work is to assess the role of breast sonography  and ductography in the evaluation of different causes of nipple discharge.

Methods :  The study will be carried out on twenty-five female patients referred to the Radiodiagnosis department at Alexandria Main University Hospital presenting with nipple discharge.

They were divided into two groups:

Group I include 10 patients (40%) with surgically significant nipple discharge who were the patients with unilateral, uniorificial surgically significant colour type nipple discharge .They were investigated by mammography, sonography, and ductography.

Group II include 15 patients

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Publication Date
Mon Feb 16 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the Level of Melatonin, Cortisol and IgA in Saliva of Patients with Oral Lichen Planus Lesions
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Back ground: Oral lichen planus is a chronic inflammatory disease that affects the mucous membrane of the mouth. Several researchers suggest that oxidative stress is implicated in the pathogenesis of this disorder. It has been hypothesized that melatonin is powerful anti-oxidants and can easily cross the cell membrane and is considered a free radical scavenger of Hydroxid, Oxygen and Nitrogen dioxide, cortisol as a stress hormone and the immunoglobulin A as first line of defense and protection to the mucous membrane of the mouth are interrelated factors for the emergence of oral lichen planus. Aim of this study was to evaluate the level of melatonin, Cortisol and IgA in saliva of patients with oral lichen planus lesions in comparison with p

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Publication Date
Wed Oct 14 2020
Journal Name
Plant Archives
EVALUATION OF THE EFFICIENCY OF SOME CHEMICAL (FYLEX), NANOPARTICLES (MGO) AND BIOLOGICAL FACTORS IN INHIBITING OF ASPERGILLUS FLAVUS
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The Fylex extract exert a high inhibition effect against A . flavus growth on PDA medium, as the fungus growth was completely inhibited by 100% at a concentration of 0.2 and 0.3% of studied extract, while the lowest inhibition percentage (71%) was found at a concentration of 0.1%. Whereas magnesium oxide nanoparticles showed the highest inhibition ratio of A. flavus (100%) was detected at 0.2% and the lowest inhibition ratio (81.66%) was at concentration 0.5%. Moreover, the addition of G. lucidum powder to PDA medium with a concentration of 2.5 mg increased the inhibition rate of A. flavus growth which was 54.4%, while the lowest inhibition ration (18.22%) was found at a concentration of 1000 mg. The milky liquid (brocade milk) of Calotropi

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Publication Date
Wed Feb 01 2017
Journal Name
Iosr Journal Of Pharmacy And Biological Sciences
Role of Diffusion Weighted MRI in Evaluation of Urinary Bladder Cancer in Iraqi Patient in Correlation with Histopathological Grade.
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Publication Date
Wed Oct 17 2018
Journal Name
Journal Of Economics And Administrative Sciences
Evaluation of Quality of Health Service in Primary Health Care Centers / Case Study in Family Medicine Centers in Baghdad
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The aim of this research is to identify the level of health services provided in the health centers operating in the family medicine system in Baghdad, and to determine the extent to which these health centers are applied to the internationally recognized standards , "Defining the quality of service gap between health care centers operating in the family medicine system and the standards adopted by the corresponding international centers (Al-Shabab Model Family Medicine Center, Al-Jahad Family Health Center, Al-Adhamiya Family Health Center, Al-Zawiya Family Health Center), and in view of what our health institutions are facing. The family of primary health care centers has difficulties, obstacles and challenges such as the diffi

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
The micronucleated erythrocytes in speeies of Iraqi fish as indieator of dilution
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The micronucleated erythrocytes in fish was used to detect water pollution by genotoxic agents. Fish belonging to different species were collected from three regions from Baghdad during three months (December/2000,January and February/2001 ).The micronucleated erythrocytes was observed in all the specimens. It was concluded that the genotoxic activity' in one region was less than in die other two regions.?

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Publication Date
Tue Jun 21 2022
Journal Name
Journal Of Planner And Development
Evaluation of some indicators of urbanization in the city of al-Qaim in the Iraqi province of Anbar
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Urban Balance is one of the important indicators that leads to an assessment of the urbanization process in a particular country  , province or even a city that is multi-centered. By examining  the data related to Anba  province, it was found that the value of this indicator is equal to 0.96, which is less than the absolute one, and therefore the urbanization in the province is distributed collectively  

The development of a mathematical or statistical model for estimating urban growth is a complex process due to the overlap between indicators or variables that can be adopted to calculate estimate growth rates Al-Qaim city has been considered as an example to develop a statistical method by which changes

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Publication Date
Thu Jun 01 2017
Journal Name
Iosr Journal Of Computer Engineering
Lossy Image Compression Using Wavelet Transform, Polynomial Prediction And Block Truncation Coding
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Publication Date
Wed Dec 25 2019
Journal Name
Journal Of Engineering
Anti-Disturbance Compensator Design for Unmanned Aerial Vehicle
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In this paper, an Anti-Disturbance Compensator is suggested for the stabilization of a 6-DoF quadrotor Unmanned Aerial vehicle (UAV) system, namely, the Improved Active Disturbance Rejection Control (IADRC). The proposed Control Scheme rejects the disturbances subjected to this system and eliminates the effect of the uncertainties that the quadrotor system exhibits. The complete nonlinear mathematical model of the 6-DoF quadrotor UAV system has been used to design the four ADRCs units for the attitude and altitude stabilization. Stability analysis has been demonstrated for the Linear Extended State Observer (LESO) of each IADRC unit and the overall closed-loop system using Hurwitz stability criterion. A minimization to a

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Publication Date
Wed Jan 01 2020
Journal Name
Biochemical And Cellular Archives
Evaluation of some immunological aspects in iraqi pregnant women with toxoplasmosis
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A total of 70 pregnant women with toxoplasmosis were studied to evaluate of some immunological aspects. The women were distributed into three groups: 37 women were IgG positive, 18 women were IgM positive and 15 women were IgG and IgM positive as well as 25 healthy women were considered as control group. Serum samples were collected and ELISA method was employed to assess levels of interleukins 4, 6, 10, Interferon gamma-induced protein 10 (IP-10), Granulocyte-macrophage colony-stimulating factor (GM-CSF) and Vascular endothelial growth factor (VEGF). As compared with control the levels of cytokines were significantly increased in serum of three pregnant women groups with toxoplasmosis and the highest increase was observed in the IgM positi

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