Preferred Language
Articles
/
mRd8LZIBVTCNdQwC3KcL
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
...Show More Authors
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.

Scopus Clarivate Crossref
View Publication
Publication Date
Sun Sep 03 2017
Journal Name
Baghdad Science Journal
Preparation and Characterization some New of Naproxen Drug Derivatives
...Show More Authors

In this research four steps of the new derivatives of Naproxen drug have been made which are known as a high medicinal effectiveness; the first step involved converting Naproxen into the corresponding ester (A) by reaction Naproxen with methanol absolute in presence H2SO4. While the second step involved treatment methyl Naproxen ester (A) with hydrazine hydrate 80% in presence of ethanol .The third reaction requires synthesis of Schiff bases (C1-C10) by condensation. of Naproxen hydrazide (B) with many substituted aromatic aldehydes . Finally, the fourth step synthesized new tetrazole derivatives ( D1- D10) by the reaction of the prepared Schiff bases (in the third step) with Sodium azide in THF as a solvent .The prepared compounds wer

... Show More
View Publication Preview PDF
Scopus (3)
Scopus Crossref
Publication Date
Mon Jun 01 2015
Journal Name
Journal Of The College Of Languages (jcl)
Emotions conflict In Balzac’s novel The Father Goriot And Stendhal’s The Red and The Black
...Show More Authors

Au XIXe siècle, avec l’excès de la passion, le roman français commence à avoir de nouvelles figures. Il tend à être un reflet de la pensée et de la passion. Stendhal et Balzac révèlent ainsi le conflit de l’âme et donnent à leur héros l’impression que tout est permis.

                Ces protagonistes doivent, d’une part, subir des fluctuations psychologiques, et d’autre part, ces héros doivent être capables de faire face aux rancunes et aux conflits destructeurs. Les personnages stendhaliens et balzaciens finissent par croire que leur combat ne portera pas ses fruits, parce que toute passion déséquilibrée mènera, soit à la fol

... Show More
View Publication Preview PDF
Publication Date
Fri Feb 17 2023
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn: 2789-3219 )
The Association of Genetic Polymorphisms in Tumor Necrosis Factor-Alpha and Interleukins with Disease Severity or Response to Biological Therapy in Iraqi Rheumatoid Arthritis Patients: A Narrative Review
...Show More Authors

Background: Tumor necrosis factor-alpha (TNF-α) and interleukins play important roles in the pathogenesis of rheumatoid arthritis (RA). Genetic research has been employed to find many of the missing connections between genetic risk variations and causal genetic components. Objective: The goal of this study is to look at the genetic variations of TNF-α and interleukins in Iraqi RA patients and see how they relate to disease severity or response to biological therapy. Method: Using specific keywords, the authors conducted a systematic and comprehensive search to identify relevant Iraqi studies examining the genetic variations of TNF-α and interleukins in Iraqi RA patients and how they relate to disease severity or response to biolo

... Show More
View Publication Preview PDF
Scopus (12)
Crossref (9)
Scopus Crossref
Publication Date
Mon May 01 2023
Journal Name
Journal Of Molecular Liquids
On the influence of hydrocarbons solvents on the inhibition efficiency of some organic corrosion inhibitors: Theoretical and validation studies
...Show More Authors

View Publication
Scopus (11)
Crossref (12)
Scopus Clarivate Crossref
Publication Date
Thu Oct 13 2022
Journal Name
Computation
A Pattern-Recognizer Artificial Neural Network for the Prediction of New Crescent Visibility in Iraq
...Show More Authors

Various theories have been proposed since in last century to predict the first sighting of a new crescent moon. None of them uses the concept of machine and deep learning to process, interpret and simulate patterns hidden in databases. Many of these theories use interpolation and extrapolation techniques to identify sighting regions through such data. In this study, a pattern recognizer artificial neural network was trained to distinguish between visibility regions. Essential parameters of crescent moon sighting were collected from moon sight datasets and used to build an intelligent system of pattern recognition to predict the crescent sight conditions. The proposed ANN learned the datasets with an accuracy of more than 72% in comp

... Show More
View Publication Preview PDF
Scopus (8)
Crossref (6)
Scopus Clarivate Crossref
Publication Date
Tue May 01 2018
Journal Name
Journal Of Engineering
Prediction of Municipal Solid Waste Generation Models Using Artificial Neural Network in Baghdad city, Iraq
...Show More Authors

The importance of Baghdad city as the capital of Iraq and the center of the attention of delegations because of its long history is essential to preserve its environment. This is achieved through the integrated management of municipal solid waste since this is only possible by knowing the quantities produced by the population on a daily basis. This study focused to predicate the amount of municipal solid waste generated in Karkh and Rusafa separately, in addition to the quantity produced in Baghdad, using IBM SPSS 23 software. Results that showed the average generation rates of domestic solid waste in Rusafa side was higher than that of Al-Karkh side because Rusafa side has higher population density than Al-Karkh side. T

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Tue Mar 20 2018
Journal Name
Day 2 Wed, March 21, 2018
Numerical Approach for the Prediction of Formation and Hydraulic Fracture Properties Considering Elliptical Flow Regime in Tight Gas Reservoirs
...Show More Authors
Abstract<p>As tight gas reservoirs (TGRs) become more significant to the future of the gas industry, investigation into the best methods for the evaluation of field performance is critical. While hydraulic fractured well in TRGs are proven to be most viable options for economic recovery of gas, the interpretation of pressure transient or well test data from hydraulic fractured well in TGRs for the accurate estimation of important reservoirs and fracture properties (e.g. fracture length, fracture conductivity, skin and reservoir permeability) is rather very complex and difficult because of the existence of multiple flow profiles/regimes. The flow regimes are complex in TGRs due to the large hydraulic fractures n</p> ... Show More
View Publication
Scopus (14)
Crossref (8)
Scopus Crossref
Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Engineering
Water Quality Assessment and Total Dissolved Solids Prediction using Artificial Neural Network in Al-Hawizeh Marsh South of Iraq
...Show More Authors

The Iraqi marshes are considered the most extensive wetland ecosystem in the Middle East and are located in the middle and lower basin of the Tigris and Euphrates Rivers which create a wetlands network and comprise some shallow freshwater lakes that seasonally swamped floodplains. Al-Hawizeh marsh is a major marsh located east of Tigris River south of Iraq. This study aims to assess water quality through water quality index (WQI) and predict Total Dissolved Solids (TDS) concentrations in Al-Hawizeh marsh based on artificial neural network (ANN). Results showed that the WQI was more than 300 for years 2013 and 2014 (Water is unsuitable for drinking) and decreased within the range 200-300 in years 2015 and 2016 (Very poor water). The develope

... Show More
Publication Date
Sun Apr 01 2018
Journal Name
Journal Of Engineering/
Water quality assessment and total dissolved solids prediction using artificial neural network in Al-Hawizeh marsh south of Iraq
...Show More Authors

The Iraqi marshes are considered the most extensive wetland ecosystem in the Middle East and are located in the middle and lower basin of the Tigris and Euphrates Rivers which create a wetlands network and comprise some shallow freshwater lakes that seasonally swamped floodplains. Al-Hawizeh marsh is a major marsh located east of Tigris River south of Iraq. This study aims to assess water quality through water quality index (WQI) and predict Total Dissolved Solids (TDS) concentrations in Al-Hawizeh marsh based on artificial neural network (ANN). Results showed that the WQI was more than 300 for years 2013 and 2014 (Water is unsuitable for drinking) and decreased within the range 200-300 in years 2015 and 2016 (Very poor water). The

... Show More
Publication Date
Wed Sep 01 2010
Journal Name
Al-khwarizmi Engineering Journal
Prediction of the Scale Removal Rate in Heat Exchanger Piping System Using the Analogies between Mass and Momentum Transfer
...Show More Authors

The possibility of predicting the mass transfer controlled CaCO3 scale removal   rate has been investigated.

Experiments were carried out using chelating agents as a cleaning solution at different time and Reynolds’s number. The results of CaCO3 scale removal or (mass transfer rate) (as it is the controlling process) are compared with proposed model of prandtl’s and Taylor particularly based on the concept of analogy among momentum and mass transfer.

Correlation for the variation of Sherwood number ( or mass transfer rate ) with Reynolds’s number have been obtained .

View Publication Preview PDF