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
Mon Jan 01 2024
Journal Name
Kafkas Universitesi Veteriner Fakultesi Dergisi
Assessment of In-vitro Cytotoxicity and In-ovo Virucidal Antiviral Efficacy of Various Plant Extracts and Bioactive Molecules
...Show More Authors

View Publication
Scopus (7)
Scopus Clarivate Crossref
Publication Date
Mon Dec 20 2021
Journal Name
Baghdad Science Journal
Recurrent Stroke Prediction using Machine Learning Algorithms with Clinical Public Datasets: An Empirical Performance Evaluation
...Show More Authors

Recurrent strokes can be devastating, often resulting in severe disability or death. However, nearly 90% of the causes of recurrent stroke are modifiable, which means recurrent strokes can be averted by controlling risk factors, which are mainly behavioral and metabolic in nature. Thus, it shows that from the previous works that recurrent stroke prediction model could help in minimizing the possibility of getting recurrent stroke. Previous works have shown promising results in predicting first-time stroke cases with machine learning approaches. However, there are limited works on recurrent stroke prediction using machine learning methods. Hence, this work is proposed to perform an empirical analysis and to investigate machine learning al

... Show More
View Publication Preview PDF
Scopus (13)
Crossref (7)
Scopus Clarivate Crossref
Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Synthesis, characterization and biological evaluation of thiazolyl azo ligand complexes with some metal ions.
...Show More Authors

(E)-2-(benzo[d]thiazol-2-yliazenyl)-4-methoxyaniline was synthesized by reaction the diazonium salt of 2-aminobenzothiazole with 4-methoxyaniline. Identified of the ligand by spectral techniques (UV-Vis, FTIR,1HNMR and LC-Mass) and microelemental analysis (C.H.N.S.O) are used to produce of the azo ligand. Complexes of (Co2+, Ni2+, Cu2+ and Zn2+) were synthesized and identified using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4-3×10-4 mole/L). height molar absorptivity of compound solutions h

... Show More
Publication Date
Mon Sep 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis, Characterization and Evaluation of Overbased Magnesium Fatty Acids Detergent for Medium Lubricating Oil
...Show More Authors

A series of overbased magnesium fatty acids such as caprylate, caprate, laurate, myristate, palmitate, stearate and oleate) were synthesized by the reaction of the fatty acids with active – 60 magnesium oxide and carbon dioxide (CO2) gas at 60 oC in the presence of ammonia solution as catalyst, toluene / ethanol solvent mixture (9:1vol/vol) was added.
The prepared detergent additives were characterized by FTIR, 1HNMR and evaluated by blending each additive in various concentrations with medium lubricant oil fraction (60 stock) supplied by Iraqi Midland Refineries Company. The total base number (TBN, mg of KOH/g) was determined, and the results of TBN were treated by using two-way analysis of variance (ANOVA) test. It was found that

... Show More
View Publication Preview PDF
Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis, Characterization and Comparative Cytotoxic Evaluation of bis-(2- mercaptoacetate) gold (III) chloride
...Show More Authors

In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.

With this frame, recently new square planar Au(III)  complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.

In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Apr 11 2019
Journal Name
Political Sciences Journal
Scientific Activities College of branches
...Show More Authors

Scientific Activities College of branches

View Publication Preview PDF
Crossref
Publication Date
Sun Dec 01 2013
Journal Name
Political Sciences Journal
Activities of International Studies Branch
...Show More Authors

نشاطات فرع الدراسات الدولية

View Publication Preview PDF
Crossref
Publication Date
Mon Dec 30 2024
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization, Thermal Studies, and Antioxidant Activities of Azo Dye[2-[(3-Hydroxyphenyl)diazinyl]-1,2-Benzothiazol-3(2H)-one-1,1-Dioxide]and Metal Ion Complexes
...Show More Authors

The new azo dye was synthesized via the reaction of the diazonium salt form of 3-aminophenol with 2-hydroxyquinoline. This dye was then used to access a series of complexes with the chlorides of manganese, iron, zinc, cadmium, and vanadium sulfate. The prepared ligand and its complexes were characterized by FT-IR spectroscopy, UV-visible spectroscopy, mass spectrometry, thermogravimetric analysis, differential scanning calorimeter, and microelemental analysis. Conductivity, magnetic susceptibility, metal content, and chlorine content of the complexes were also measured. The ligand and cadmium complex were identified using1H NMR and 13C NMR spectroscopy. The results showed that the shape of the ligand is a trigonal planner, and the c

... Show More
View Publication
Scopus (10)
Scopus Crossref
Publication Date
Thu Mar 31 2016
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Permeability Prediction in One of Iraqi Carbonate Reservoir Using Hydraulic Flow Units and Neural Networks
...Show More Authors

Permeability determination in Carbonate reservoir is a complex problem, due to their capability to be tight and heterogeneous, also core samples are usually only available for few wells therefore predicting permeability with low cost and reliable accuracy is an important issue, for this reason permeability predictive models become very desirable.

   This paper will try to develop the permeability predictive model for one of  Iraqi carbonate reservoir from core and well log data using the principle of Hydraulic Flow Units (HFUs). HFU is a function of Flow Zone Indicator (FZI) which is a good parameter to determine (HFUs).

   Histogram analysis, probability analysis and Log-Log plot of Reservoir Qua

... Show More
View Publication Preview PDF
Publication Date
Sat Jun 28 2014
Journal Name
Iraqi Postgraduate Medical Journal
Comparism Between Transvaginal Cervical Length Measurement and Digital Examination in Prediction of Imminent preterm Delivery
...Show More Authors

BACKGROUND: Preterm labour is a major cause of perinatal morbidity and mortality, so it is important to predict preterm delivery using the clinical examination of the cervix and uterine contraction frequency. New markers for the prediction of preterm birth have been developed such as transvaginal ultrasound measurement of cervical length as this method is widely available. OBJECTIVE: To determine, whether transvaginal cervical length measurement predicts imminent preterm delivery better than digital cervical length measurement in women presented with preterm labour and intact membranes. PATIENTS AND METHODS: Two hundred women presented with preterm labour between 24 and 36+6 weeks of gestation were included in this study. All women subjecte

... Show More
View Publication