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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 04 2019
Journal Name
Journal Of The College Of Education For Women
Root (GUM) and its derivatives between Lexical Sematics and Semantics Koranic
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As the word can fluctuate between central and peripheral dlalten it represents the first lexical meaning and the second represents the meaning that gain by the context in which it appear so this research came to show signs that can be acquired the root ( GUM ) and its derivatives from the contexts in which it is mentioned in the Koran as well as siqnificant Lexical if this research is divided on two first is eating Lexical semantics , the second handled connotations in the Koran was based on what the commentators and concemed with the meanings of the Koran and the owners Almagamat in astatement that the semantic .

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Publication Date
Mon Aug 19 2024
Journal Name
Journal Of Metastable And Nanocrystalline Materials
The Structural, Magnetic, and Electrochemical Properties of Composite PAni/Co<sub>0.2</sub>Mn<sub>0.8</sub>Fe<sub>2</sub>O<sub>4</sub>
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The current work concerns preparing cobalt manganese ferrite (Co0.2Mn0.8Fe2O4) and decorating it with polyaniline (PAni) for supercapacitor applications. The X-ray diffraction findings (XRD) manifested a broad peak of PAni and a cubic structure of cobalt manganese ferrite with crystal sizes between 21 nm. The pictures were taken with a field emission scanning electron microscope (FE-SEM), which evidenced that the PAni has nanofibers (NFs) structures, grain size 33 – 55 nm, according to the method of preparation, where the hydrothermal method was used. The magnetic measurements (VSM) that were conducted at room temperature showed that the samples had definite magnetic properties. Additionally, it was noted that the saturation magnetizatio

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Publication Date
Thu Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Prediction of Performance Equations for Household Compressors Depending on Manufacturing Data for Refrigerators and Freezers
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Abstract

 A surface fitting model is developed based on calorimeter data for two famous brands of household compressors. Correlation equations of ten coefficient polynomials were found as a function of refrigerant saturating and evaporating temperatures in range of (-35℃ to -10℃) using Matlab software for cooling capacity, power consumption, and refrigerant mass flow rate.

Additional correlations equations for these variables as a quick choice selection for a proper compressor use at ASHRAE standard that cover a range of swept volume range (2.24-11.15) cm3.

The result indicated that these surface fitting models are accurate with in ± 15% for 72 compressors model of cooling cap

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Publication Date
Thu Jan 03 2019
Journal Name
International Journal Of Civil Engineering And Technology (ijciet)
Condition Prediction Models of Deteriorated Trunk Sewer Using Multinomial Logistic Regression and Artificial Neural Network
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Sewer systems are used to convey sewage and/or storm water to sewage treatment plants for disposal by a network of buried sewer pipes, gutters, manholes and pits. Unfortunately, the sewer pipe deteriorates with time leading to the collapsing of the pipe with traffic disruption or clogging of the pipe causing flooding and environmental pollution. Thus, the management and maintenance of the buried pipes are important tasks that require information about the changes of the current and future sewer pipes conditions. In this research, the study was carried on in Baghdad, Iraq and two deteriorations model's multinomial logistic regression and neural network deterioration model NNDM are used to predict sewers future conditions. The results of the

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Publication Date
Thu Oct 01 2020
Journal Name
Journal Of Engineering Science And Technology
Water quality assessment and sodium adsorption ratio prediction of Tigris River using artificial neural network
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Publication Date
Thu Oct 01 2020
Journal Name
Journal Of Engineering Science And Technology (jestec)
Water Quality Assessment and Sodium Adsorption Ratio Prediction of Tigris River Using Artificial Neural Network
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Sodium adsorption ratio (SAR) is considered as a measure of the water suitability for irrigation usage. This study examines the effect of the physicochemical parameters on water quality and SAR, which included Calcium(Ca+2), Magnesium(Mg+2), Sodium (Na+), Potassium (K), Chloride (Cl-), Sulfate(SO4-2), Carbonate (CO3-2), Bicarbonate (HCO3-), Nitrate (NO3-), Total Hardness (TH), Total Dissolved Salts (TDS), Electrical Conductivity (EC), degree of reaction (DR), Boron (B) and the monthly and annually flow discharge (Q). The water samples were collected from three stations across the Tigris River in Iraq, which flows through Samarra city (upstream), Baghdad city (central) and the end of Kut city (downstream) for the periods of 2016-201

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Publication Date
Mon Apr 01 2013
Journal Name
International Journal Of Drug Development And Research
Therapeutic potential effects of pyridoxine and /or ascorbic acid on microalbuminuria in diabetes mellitus patient's: A randomized controlled clinical study
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Objectives: This study aimed to evaluate the therapeutic potential effects of ascorbic acid or and pyridoxine on diabetic renal microalbumiuria. Methods: This was a cross-sectional study on patients with diabetes mellitus at Al-Yarmouk teaching hospital from January to December 2012, Iraq-Baghdad. Twenty one patients with diabetes mellitus (D.M), 8 IDDM and 13 IDDM were selected from, the duration of disease were ranged from 2-12 years for both type (10 females and 11males) and all enrolled patients ages were ranged from 28-65years. The concentration of total protein in urine was calculated by a biuret colorimetric assay and the urine creatinine level was measured by a modified Jaffe test. Statistical analysis: results are expressed as mean

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Scopus
Publication Date
Tue Jun 15 2010
Journal Name
International Journal Of Poultry Science
Effect of n-3 and n-6 Fatty Acid Supplemented Diets on Semen Quality in Japanese Quail (Coturnix coturnix japonica)
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Crossref (25)
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Publication Date
Thu Dec 31 2020
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EVALUATION OF ELECTRONIC TRADING AND CENTRAL DEPOSITERY IN THE IRAQ STOCK EXCHANGE FOR THE PERIOS (2008- 2018): EVALUATION OF ELECTRONIC TRADING AND CENTRAL DEPOSITERY IN THE IRAQ STOCK EXCHANGE FOR THE PERIOS (2008- 2018)
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The rapid developmemt of information technology and its use in all fields has a bositive influence on all fields , and financial markets have a share of this development through the use of an electronic trading system to settle transactions and enhance transparency and disclosure in all activities of these markets and stimulate their performance .

It is worth nothing that these revolutions remove the necessity for nonstop connection with persons through the internet or phone networks , novel knowledge decreases the charges of structure original transaction system and reducing the fences of new participants entry .

The development in transportations expertise allows for quicker or

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Publication Date
Thu Jul 11 2019
Journal Name
Journal Port Science Research
Evaluation Activity of Alanine Aminopeptidase (AAP) in Patients with Renal Dialysis, Purification and Isolation of Isoenzymes
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