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Synthesis, Molecular Docking Study and Cytotoxicity Evaluation of some Quinazolinone Derivatives as Nonclassical Antifolates and Potential Cytotoxic Agents
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Abstract

A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized   by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most potent one is compound S2 (IC50: 5.73 µM). Among the tested compounds, compound S1 exhibited the highest antitumor activity against MCF-7cell line (IC50: 3.38 µM) compared to MTX (IC50: 27.32 µM). The binding modes of the synthesized compounds with the target proteins (DHFR and TS) were investigated by molecular docking studies using GOLD software.

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Publication Date
Sun Apr 02 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Conjugation of Steroidal and Non – Steroidal Anti- Inflammatory Drugs as Possible Mutual Prodrug
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Prednisolone (SAID) was conjugated with ibuprofen (NSAID) through an amino acid (glycine) as a spacer arm to synthesize the following compound:

Prednisolone – glycine – ibuprofen.

    The method employed consists of converting the carboxylic acid function of (R,S) – ibuprofen – glycine to the highly reactive acid chloride and subsequent reaction with the C21 hydroxyl group of prednisolone. This reactive intermediate was found to react as well with the C17 tertiary hydroxyl group of the steroid to form three compounds and eight diastereomers. These results were confirmed by T.L.C, and the desired compound was separated by column chromatograph

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Publication Date
Thu Mar 18 2021
Journal Name
Journal Of Research In Medical And Dental Science
Antibacterial Activity of Bioactive Glass 45S5 and Chitosan Incorporated as Fillers into Gutta Percha
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Antibacterial Activity of Bioactive Glass 45S5 and Chitosan Incorporated as Fillers into Gutta Percha, Ahmed I AL-Jobory*, Raghad AL-Hashimi

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Publication Date
Thu Feb 15 2018
Journal Name
International Journal Of Architectural Heritage
Active use of panoramic mobile mapping systems for as built surveying and heritage documentation
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Publication Date
Thu Apr 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Effect of Metals ( Au, Ag, and Ni) as Cathode Electrode on Perovskite Solar Cells
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Abstract<p>Gold, silver and nickel used as electrodes in the fabrication of perovskite solar cell by using thermal evaporation deposition method with direct structure FTO\ TiO<sub>2</sub>\ MAPbI<sub>3</sub>\ spiro-MeOTAD\ metal electrode. The cell efficiency was compared between the electrodes material as a function of time to explaining the effect of these metals electrode on cell performance, X-ray diffraction pattern showed that the samples that contain gold and nickel do not contain a compound indicating the interaction of the metal with the components of the cell or the formation of a new compound, while in the cell containing silver it was found that silver iodide is fo</p> ... Show More
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Publication Date
Wed Aug 30 2023
Journal Name
Biomedicine
Gene expression of Interleukin-10 and Foxp3 as critical biomarkers in rheumatoid arthritis patients
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Introduction and Aim: Forkhead box P3 (FOXP3) and interleukin-10 (IL-10) are the key regulators controlling the activity of Treg cells, which are crucial for maintaining immune tolerance and reducing autoimmune reactions. The objective of this study was to investigate the potential utility of elevated levels of FOXP3 and IL-10 gene expression as a diagnostic indicator in patients with rheumatoid arthritis (RA).   Materials and Methods: The study used quantitative polymerase chain reaction (qPCR) to examine the expression levels of FOXP3 and IL-10 transcripts in whole blood samples from Iraqi patients with rheumatoid arthritis. A group of healthy control subjects were also included in the study.   Results: In blood samples taken fr

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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Montelukast Sodium ( SMLT ) as a Dual Sustained Release Buccal Strips
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An oral bi layer  sustained release (SR) strips of Sodium  Montelukast SMLT , which is selective  leukotriene  antagonist  , used  for  patients  suffered from mid-night asthma , were prepared successfully ,using different polymers, like guar  gum , carrageenan , and xanthan gum , by solvent casting method .

The results obtained by this study revealed  ,that best  fast  dissolving  film of  SMLT was  loaded  in carrageenan   polymer 57%  w\w (30mg.) ,  with  acceptable  physical properties, like film thickness , elastic endurance and  surface pH  .

Besides  to that , the  disintegration  t

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Publication Date
Sun Jul 31 2022
Journal Name
Iraqi Journal Of Science
Adsorption of Biebrich Scarlet Dye into Remains Chromium and Vegetable Tanned Leather as Adsorbents
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Chromium tanned leather wastes (CTLW) and vegetable tanned leather wastes (VTLW) were used as adsorbent materials to remove the Biebrich scarlet dye (BS), as an anionic dye from wastewater, using an adsorption method. The effects of various factors, such as weight of leather waste, time of shaking, and the starting concentration of Biebrich scarlet dye, temperature and pH were studied. It described the adsorption process using Langmuir and Freundlich isotherm models. The obtained results agreed well with the Langmuir model, and the maximum adsorption capacities of CTLW and VTLW were 73.5294 and 78.1250 mg.g⁻¹, respectively, suggesting a monolayer adsorption process. The adsorption kinetic was found to follow a pseudo-second-order kinetic

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Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Study of Nutritional Adequacy Provided by some Imported Infant Milk Formula Available in the Local Market: Study of Nutritional Adequacy Provided by some Imported Infant Milk Formula Available in the Local Market
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Abstract:
This investigation was carried out to study the nutritional adequacy for
infant milk formula, which imported by Iraqi Ministry of Trade, and are
available in local markets .Most of these formulas contained nearly the same
composition of nutrients which are ,Matines ,Sunny Boy , Salsabeel AL- Badie
,Moroug, ,Charton ,Materna Lery Celia ,Lacstar Lailac,Nactalia. yet they are
unbalanced for providing the daily nutritional requirements for infants whom
depend on bottle feeding for six times daily in their first six month of age. As
there were an increase in daily intake for protein content and most vitamins
that included D, E, C, B1, B2, Niacin, B6, B12, and Biotin as well as most
minerals namely Calci

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Publication Date
Fri Mar 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
An empirical Evaluation of the effect of service encounter on customer voluntary behavior: Exploration study of (TBI) customers
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Purpose: To determine the impact of service encounter in stimulating voluntary customer behaviors.

  • Approach / methodology: It was selected a sample of customers Bank Iraqi Trade (TBI) was (105) individual, using a questionnaire designed in the light of previous studies, was drafted scale and tested in the light of a group of statistical methods developed (reliability coefficient, reliability coefficient composite, convergence). Then test hypotheses through structural equation modeling.
  • Results: The behaviors and characteristics of the service provider in effect urged bank customers to perform voluntary extra, as the service environment service encounter

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Publication Date
Wed Jul 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion
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Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.

 ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.

Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas

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