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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 Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
The Application of the Alternative Evaluation Strategy in Social Studies In General Education in KSA
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The study aims to reveal the degree of application of the alternative evaluation strategy in social studies in public education in the Kingdom of Saudi Arabia. It also aims to identify the opinions of experts on how to implement this. The study adopted the mixed methodology, which represented in the descriptive-analytical method, and qualitative methods through the grounded theory. The study used two tools namely: a questionnaire for assessments of social studies teachers and semi-structured interview questions. The results of the study showed a medium degree of appreciation for the application of alternative evaluation strategies by social studies teachers in general education with an average of (2.28). The results also showed that ther

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Publication Date
Sun Mar 01 2020
Journal Name
Plant Archives
EVALUATION THE ACTIVITY OF SOME MEDICINAL PLANTS EXTRACTS AS PROMOTER ROOTING FOR STEM CUTTINGS OF ROSEMARY (ROSMARINUS OFFICINALIS L.)
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This study was conducted in the botanical garden, Department of biology, College of Science / Mustansiriyah University in spring season, where the starts from (15 February to 15 March, 2019). Under the natural environmental conditions in the greenhouse in order to evaluate the effectiveness of some plant extracts as a promoter for rooting the apical stem cutting of rosemary plants at different concentrations compared with the IBA growth regulator. Plant extracts are Parsley (Petroselinum crispum), Dill (Anethum graveolens) and date palm fruits (Phoenix dactylifera) were used with concentrations (0, 1.25, 2.5 g / l). The IBA concentration was (100 mg / L) with dipping time 24 hour for all treatments. The following measurements were taken aft

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Publication Date
Tue Aug 22 2023
Journal Name
Microbial Science Archives
Unveiling Westiellopsis akinetica: a novel species in the Iraqi habitat, and contrasting its distinctive attributes with Westiellopsis prolifica
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This is the first record of a new species of cyanobacteria Westiellopsis akinetica in the Iraqi environment, Samples were collected on June 2013 and the existence of it was not documented before. We isolated and purified this species ten years ago in Iraq, but we couldn't identify accurately based on all taxonomic handbooks. This is due to the species features being different from the other documented species in the available taxonomic lectures. It resembled many species by morphological characteristics such as Fischerella muscicola, Fischerella thermalis, Westiellopsis biateralis SA16. Westiellopsis interrupta, Westiellopsis persica SA33, Westiellopsis prolifica and Symphyonema bifilamentata. Describing a new species of the Westiellops

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Publication Date
Sun Feb 15 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The value of ultrasound and color Doppler ultrasonography in the evaluation of periapical lesions in comparison to histopathological and/or surgical findings
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Background: Imaging techniques play a very important role in the specialty of endodontic. The ultrasonographic technique is non-expensive procedure, safe, and reproducible. The aim of the study was to determine the sensitivity, specificity, and accuracy of ultrasound and color Doppler ultrasonography in evaluation of periapical lesions (cyst, granuloma, mixed lesion “cyst within graulomas mass”, and abscess. Subject, Material and method: The sample consists of prospective study for 64 Iraqi participants who attended Karbalaa Specialized Center for Dentistry (males & females). Those patients were diagnosed clinically and radiographically as having periapical lesions of dental origin. They were examined by real time ultrasound and color

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Different Concentrations of Melatonin on the Time-course of Nitrite–induced Oxidation of Hemoglobin: In vitro Study
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         Melatonin is a potent scavenger of reactive oxygen species or free radicals like superoxide and hydroxyl radicals. The oxidation of hemoglobin to methemoglobin (meth-Hb) by oxidizing compounds has been widely studied. The present work was designed to evaluate the ability of different concentrations of melatonin to inhibit nitrite–induced oxidation of hemoglobin. Blood samples were obtained from apparently healthy individuals from which erythrocyte hemolysate was prepared. Different concentrations of melatonin (10-9-1.0 mg/ml) were incubated for 10 min with the hemolysate, then to the resultant mixture 1 ml of sodium nitrite (final concentration 0.6 mM) was added, and the

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Crossref
Publication Date
Thu Jun 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Effects of Two Different Colorant Solutions on the Color Stability of Bleached Enamel in Association with CPP-ACPF: An In Vitro Study
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Background: One of the drawbacks of vital teeth bleaching is color stability. The aim of the present study was to evaluate the effects of tea and tomato sauce on the color stability of bleached enamel in association with the application of MI Paste Plus (CPP-ACPF). Materials and Methods: Sixty enamel samples were bleached with 10% carbamide peroxide for two weeks then divided into three groups (A, B and C) of 20 samples each. After bleaching, the samples of each group were subdivided into two subgroups (n=10). While subgroups A1, B1 and C1 were kept in distilled water, A2, B2, and C2 were treated with MI Paste Plus. Then, the samples were immersed in different solutions as follow: A1 and A2 in distilled water (control); B1 and B2 in black

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Crossref
Publication Date
Wed Sep 20 2023
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Bioactivity Evaluation for Some Metal Ions Complexes with New Ligand Derived from 2-hydroxy-1- napthaldehyed
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The newly synthesized Schiff base ligand (E)-2-((2-phenylhydrazono)methyl)naphthalen-1-ol (phenyl hydrazine derivative), is allowed to react with each of the next mineral ion: Ni2+, Cu2+, Zn2+andCd2+successfully resulting to obtain new metal complexes with different geometric shape. The formation of Schiff base complexes and also the origin Schiff base is indicated using LC-Mass that manifest the obtained molar mass, FT-IR proved the occurrence of coordination through N of azobenzene and O of OH by observing the shifting in azomethines band and appearing of M-N and N-O bands. Moreover, we can also detect by such apparatus, the presence of aquatic water molecule inside the coordination sphere. UV-Vis spectra of all resultants reveale

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Publication Date
Thu Oct 01 2009
Journal Name
Jssdds
Topical 10% lactic acid solution in the treatment of pityriasis versicolor in comparison with topical 1% clotrimazol solution (single-blind, comparative and therapeutic study)
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KE Sharquie, AA Noaimi, AM Oweid, JSSDDS, 2009 - Cited by 2

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Publication Date
Sun Sep 01 2024
Journal Name
Iraqi Journal Of Physics
Synthesis of PPy-MnO2 Nanocomposite for Utilization in Supercapacitor Applications
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Polypyrrole (PPy) nanocomposites were prepared using chemical oxidation and were combined with manganese oxide (MnO2) nanoparticles. The PPY-MnO2 nanocomposite was synthesized by integrating PPy nanofibers with varying volume ratio percentages of MnO2 dopant (10, 30, and 50% vol. ratio). The structural features of the PPy and PPy-MnO2 nanocomposite were investigated using X-ray diffraction (XRD).  Fourier transfor infrared (FTIR) spectroscopy was used to demonstrate the molecular structures of primary materials and the final product of PPy, MnO2, and PPy- MnO2 nanocomposites. Field Emission Scanning Electron Microscopy (FESEM) showed that the morphology of PPy consisted of a network of nanofibers. Increasing the volume ratios of ma

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Crossref
Publication Date
Tue Dec 06 2022
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Blended Learning in Nursing Education at the Middle Region in Iraq
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Abstract

Objective(s): To evaluate blended learning in nursing education at the Middle Region in Iraq.

Methodology: A descriptive study, using evaluation approach, is conducted to evaluate blended learning in nursing education in Middle Region in Iraq from September 26th, 2021 to March 22nd, 2022. The study is carried out at two Colleges of Nursing at the University of Baghdad and University of Tikrit in Iraq. A convenient, non-probability, sample of (60) undergraduate nursing students is selected. The sample is comprised of (30) student from each college of nursing, Self-report questionnaire is constructed from the literature, for e

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