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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
Wed Jul 13 2022
Journal Name
International Journal Of Health Sciences
Study of the reliability of serum vascular endothelial growth factor and its soluble receptor as markers of diabetic nephropathy in type 2 diabetes patients
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The levels of circulating angiogenic and anti-angiogenic factors, namely vascular endothelial growth factor–A (VEGF-A) and soluble vascular endothelial growth factor receptor-1 (sVEGFR-1), have been linked to the development of renal dysfunction due to the proliferation of microvasculature within the kidneys of type 2 diabetic (T2DM) patients. The study aims to scrutinize serum levels of VEGF and sVEGFR-1 in a sample of Iraqi diabetic nephropathy patients to support their reliability as markers for the prediction of nephropathy in type 2 diabetes mellitus patients as well as to assess the ACE inhibitor’s effect on the levels of these two markers. Method: The ninety participants of this case-control study were split into three gr

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Publication Date
Sat Mar 01 2025
Journal Name
Microbial Biosystems
Distribution of cytotoxic necrotizing factor type 1 in clinical isolates of Escherichia coli isolated from urinary tract infections in Iraq
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Uropathogenic Escherichia coli is the main cause of urinary tract infections, the ability of this bacteria to cause urinary tract infections is related to a variety of virulence factors that enhance colonization and evade the immune response, one of these virulence factors is cytotoxic necrotizing factor 1 toxin which converts the glutamine residue to glutamic acid to activated GTPase Rho family. The study was meant to find out the prevalence rate of the cnf1 gene in Uropathogenic Escherichia coli isolated from Iraqi patients. Conventional laboratory methods were used for primary bacterial identification and molecular methods were used to confirm bacterial identity and gene detection. Escherichia coli was identified in 89/165 (53.93%) of th

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Publication Date
Sat Jun 29 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Characterization of New 5-Fluoroisatin-Chalcone Conjugates with Expected Antimicrobial Activity
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Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemic

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Publication Date
Tue Jun 30 2020
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EVALUATION OF SPORTS AWARENESS AMONG WOMEN AT THE UNIVERSITY OF BAGHDAD FOR THE PERIOD 2011-2016 AND STUDY THE FACTORS AFFECTING THEIR PARTICIPATION IN SPORTS ACTIVITIES: EVALUATION OF SPORTS AWARENESS AMONG WOMEN AT THE UNIVERSITY OF BAGHDAD FOR THE PERIOD 2011-2016 AND STUDY THE FACTORS AFFECTING THEIR PARTICIPATION IN SPORTS ACTIVITIES
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The exercise of activities and sports are of great importance to public health and to maintain the ideal health weight as well as the psychological and mental comfort of humans. The aim of this study is to determine the contribution and participation of educated females in physical activities at the University of Baghdad hall for the years 2011-2016, and to show the factors that influence women's contribution to physical activities at the university by selecting 100 students of males and 100 females' students randomly. During the questioning questions and statistical analysis of the questioning to find out the reasons for the discouraging contribution of the women to the various physical activities and try to find solutions and r

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Publication Date
Wed Jan 25 2012
Journal Name
Synthesis, Characterization And Antibacterial Activities Of Some Metal (ii) Heterocyclic Polyamine Complexes With 6,6'-(1,4-phenylenebis(azanediyl) Bis(2- Amino-6-methyl-6h-1,3-oxazin-4-ol) Ligand.
Synthesis, characterization and Antibacterial activities of some metal (II) heterocyclic polyamine complexes with 6,6'-(1,4-phenylenebis(azanediyl) bis(2-amino-6-methyl-6H-1,3-oxazin-4-ol) ligand.
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Publication Date
Mon Jan 01 2018
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
A Sensitive Electrochemical Sensor for Rapid Determination of Mebeverine Hydrochloride and Metronidazole Benzoate Selective Molecular Imprinted Polymer in the PVC Membrane
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Publication Date
Sat Dec 20 2025
Journal Name
Bulletin Of The Iraq Natural History Museum
MORPHOLOGICAL AND MOLECULAR DESCRIPTION FOR A NEW RECORD OF NEMATODE ACROBELOIDES VARIUS KIM, KIM & PARK, 2017 (RHABDITIDA, CEPHALOBIDAE) FROM IRAQ
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This study aimed to identify and describe one of the bacterial feeder nematode Acrobeloides varius Kim, Kim and Park, 2017 (Rhabditida, Cephalobidae), which was isolated from soil samples that were collected from Baghdad, central of Iraq, and was classified using both morphological and molecular criteria. All specimens of A. varius were cultured, identified and described using morphometric criteria. Selected specimens (Zah. IRQ3 OR994579.1 isolate) of this species were characterized by having the body length of the male ranging from (184.94 – 221.72 μm), the body length of the female ranging (507.38 – 521.92 μm) and the body length of the juvenile ranging from (355.53 – 490.35 μm). Selected specimens of this species were m

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Publication Date
Mon Aug 01 2022
Journal Name
Azerbaijan Medical Journal
Molecular Co- Localization of Human Papilloma Virus 6 / 11 in Combined Resected Tissues from Nononcologic Palatine and Pharyngeal Tonsillar Hypertrophies
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More than 450 distinct types of human papilloma virus recognized via recent molecular techniques. The low and high oncogenic risk-HPV genotypes have an association with a variety of benign and malignant tumors in the oropharyngeal and nasopharyngeal localizations. This study aimed to determine the rate of DNA detection of HPV genotype 6/11 in non-oncologic nasopharyngeal and palatine tonsillar tissues from pediatric patients subjected to adeno-tonsillectomies. A total number of 64 tissue specimens enrolled; 44 non-oncologic nasopharyngeal and palatine hypertrophied tissue specimens from 22 pediatric patients sustained combined adeno-tonsillectomies and compared to 20 nasal trimmed tissues with unremarkable pathological changes (in

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Publication Date
Fri Aug 15 2025
Journal Name
Baghdad Science Journal
Hydrothermal synthesis of high surface area mesoporous silica as an efficient adsorbent for removal of crystal violet dye from aqueous solution
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Publication Date
Fri Aug 15 2025
Journal Name
Baghdad Science Journal
Hydrothermal synthesis of high surface area mesoporous silica as an efficient adsorbent for removal of crystal violet dye from aqueous solution
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