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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 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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Crossref
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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Crossref
Publication Date
Fri Jan 01 2021
Journal Name
Bionatura
STUDY THE TIGRIS RIVER IN SOUTH OF BAGHDAD CITY AND MAY USE IT AS IRRIGATION WATER
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Scopus
Publication Date
Thu Dec 15 2022
Journal Name
Al-academy
Discourse the presence of animals in Mesopotamian sculptures "The lion and the bull as an example"
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Showing animal shapes is one of the primary topics since the discovery of cave drawings, with semantic discourses, as they appeared in the ancient civilization of Iraq, with their discourse and intellectual structure, and their reflections on their plastic achievements. The research deals with three topics: the first (an introduction to the concept of discourse), the second: (the historical roots of animal forms), and the third (the manifestation of animal forms and their discourse, in Mesopotamia). Mesopotamian fauna and its concepts? What are the?, Its importance was also represented in: the presence of animals and their semantic and conceptual discourse, especially the sculptures (the lion and the bull), with the aim of revealing the

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Crossref
Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Fabrication of PVC Enrofloxacin-Selective Electrodes for Estimating Enrofloxacin in Pure Form and as Preparation Formula:
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This study explored the development and qualities of the response of electrochemical properties of enrofloxacin-selective electrodes using precipitation based on producing phosphotungstic, after utilizing a matrix of polyvinyl chloride (PVC) and dibutyl phthalate or dibutyl phosphate as a plasticizer. The resulting membrane sensors were an enrofloxacin-phosphotungstic electrode (sensors 1) and an ENR-DOP-PTA electrode (sensors 2). Linear responses of (ENR-DBPH-PTA) and (ENR-DOP-PTA) within the concentration ranges of 2.1×10-6-10-1 and 3.0×10-6-10-2 mol. L-1, respectively, for both sensors were observed. Slopes of 51.61±0.24 and 39.40± 0.16 mV/decade and pH ranges equal to 2.5-8.5

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Publication Date
Sun Apr 02 2023
Journal Name
Journal Of Survey In Fisheries Sciences
Evaluation of the Serum Asprosin Levels in Patients with Double Diabetes
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Background : Double diabetes (DD) is the term used to describe situations in which a patient exhibits characteristics that are a combination of type 1 diabetes mellitus(T1DM) and type 2 Diabetes Mellitus (T2DM) a large epidemiological study found that 25.5% of people with T1D also had the metabolic syndrome. A new protein hormone called asprosin is predominantly released by white adipose tissue. It was initially discovered in 2016 . Asprosin is important diagnoses marker for insulin resistant in diabetes patients ,additionally is very important denotation about early diagnoses of type 2 diabetes. Objectives: The current study aims to find predictive significance of diagnosis a double diabetes by evaluating the asprosin in the blood serum of

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Publication Date
Sat Feb 01 2014
Journal Name
Journal Of Engineering
Assessment Efficiency Evaluation of Al-Diwaniya Sewage Treatment Plant in Iraq
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This study aims to evaluate the performance of the sewage treatment plant in Al- Diwaniya, one of cities in the southern part in Iraq. This evaluation could be used to facilitate effluent quality assessment or optimal process control of the plant. The influent reaching the plant is considered a medium to strong in strength with BOD5/COD ratio in the range 0.23 and 0.69 which can be considered an easily degradable sewage by the biological processes performed by the activated sludge unit. The quality of the effluent was found to be higher than the Iraqi standards for disposal to water bodies. The BOD5/COD ratios of the treated sewage varied over a wide range as low of 0.13 to 1.48 indicating operational problems in the plant. Regressio

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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Hepatic Enzymes in major β-thalassemic Patients using Deferasirox
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Abstract

β-thalassemia major is a genetic disease that causes sever defect in normal hemoglobin synthesis. The patients with β-thalassemia major need periodic blood transfusions that can result in accumulation of body iron, so treatment with iron chelating agent is required. Complications of this iron overload affecting many vital organs, including the liver. The aim of this work was to evaluate liver enzymes in β -thalassemia major patients with deferasirox versus without it. Two groups of β-thalassemia major patients were involved in this study named group A; 40 β-thalassemia patients of blood transfusion dependent without deferasirox, group B; 40 β-thalassemia patients of blood transfusion dependent on de

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Publication Date
Mon Jan 01 2018
Journal Name
Matec Web Of Conferences
Evaluation water quality of Diyala River in Iraq using Bhargava method
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Diyala River is a tributary of Tigris River, it is one of the important rivers in Iraq. It covers a total distance of 445 km (275 miles). 32600 km2is the area that drains by Diyala River between Iraqi-Iranian borders. This research aims to evaluate the water quality index WQI of Diyala River, where three stations were chosen along the river. These stations are D12 at Jalawlaa City at the beginning of Diyala River, the second station is D15 at Baaquba City at the mid distance of the river, and the third station is D17 which is the last station before the confluence of Diyala River with Tigris River at Baghdad city. Bhargava method was used in order to evaluate the water quality index for both irrigation and drink

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Publication Date
Thu Nov 08 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of nurses' practices toward postoperative wound dressing in surgical wards
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Objective(s): The study aimed to assess the level of nursing performance and practices in terms of approaching or
distancing itself from the optimal performance criteria universally adopted within the variable dressing surgical
wounds of patients admitted to the surgical wards, and determine the relationship between the level of nurse's
performance and socio-demographic characteristics of them in those wards.
Methodology: A descriptive assessing design was adopted from November the 10th, 2010 until June the 1st, 2011 to
assess the nursing care provided practices for the postoperative period within the variable dressing surgical wounds in
the complex of Medical City. Whereas the study was conducted in three hospitals; Ba

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