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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
Tue Jul 01 2025
Journal Name
Russian Journal Of Physical Chemistry A
Electrochemical and Theoretical Study of the Corrosion Inhibition of Carbon Steel Using 3-Allyl-2-mercaptoquinazolin-4(3H)-one in an Acidic Environment
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This study investigates the corrosion inhibition performance of a newly synthesized quinazolinone derivative, AMQ, on mild steel in a hydrochloric acid medium. The inhibition efficiency was evaluated using potentiodynamic polarization at varying inhibitor concentrations (100–250 ppm) and temperatures (303– 333 K). The results showed that AMQ exhibited effective corrosion inhibition, with the highest efficiency of 74% observed at 250 ppm and 323 K. Density Functional Theory (DFT) calculations were conducted to study the electronic properties of AMQ and its adsorption behavior. The thermodynamic parameters, including activation energy, enthalpy, and Gibbs free energy, were calculated, indicating spontaneous adsorption of AMQ onto the meta

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of the Clinical use of Metformin or Pioglitazone in Combination with Meloxicam in Patients with Knee Osteoarthritis; using Knee Injury and Osteoarthritis outcome Score
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Osteoarthritis is the most prevalent arthritic disease and a leading cause of disability. The pathogenesis of osteoarthritis involves multiple etiologies, including variable degree of synovial inflammation. Metformin and pioglitazone could potentially reduce the levels and activity of inflammatory mediators. This may consider as a new therapeutic approach added to the current used drugs in an attempt to decrease the pain, inflammation, and improve daily activity and quality of life in patients with knee osteoarthritis.

This study designed to evaluate the clinical utility of using metformin or pioglitazone as anti-inflammatory agents in combination with non-steroidal anti-inflammatory drugs (NSAID) of selective type of cyclooxygen

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Publication Date
Wed Sep 11 2024
Journal Name
Lecture Notes In Civil Engineering
An Image Processing Algorithm to Address the Problem of Stains Merge on Water Sensitive Papers and Its Impact on the Evaluation of Spray Quality Indicators
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There are many techniques that can be used to estimate the spray quality traits such as the spray coverage, droplet density, droplet count, and droplet diameter. One of the most common techniques is to use water sensitive papers (WSP) as a spray collector on field conditions and analyzing them using several software. However, possible merger of some droplets could occur after they deposit on WSP, and this could affect the accuracy of the results. In this research, image processing technique was used for better estimation of the spray traits, and to overcome the problem of droplet merger. The droplets were classified as non-merged and merged droplets based on their roundness, then the merged droplets were separated based on the average non-m

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Publication Date
Thu Mar 02 2023
Journal Name
East European Journal Of Physics
Evaluation of the Influence of Body Mass Index and Signal-to-Noise Ratio on the PET/CT Image Quality in Iraqi Patients with Liver Cancer
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Image quality has been estimated and predicted using the signal to noise ratio (SNR). The purpose of this study is to investigate the relationships between body mass index (BMI) and SNR measurements in PET imaging using patient studies with liver cancer. Three groups of 59 patients (24 males and 35 females) were divided according to BMI. After intravenous injection of 0.1 mCi of 18F-FDG per kilogram of body weight, PET emission scans were acquired for (1, 1.5, and 3) min/bed position according to the weight of patient. Because liver is an organ of homogenous metabolism, five region of interest (ROI) were made at the same location, five successive slices of the PET/CT scans to determine the mean uptake (signal) values and its standard deviat

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Publication Date
Wed Mar 30 2022
Journal Name
Journal Of Educational And Psychological Researches
The degree of using electronic educational alternatives in education from the teachers 'and female teachers' point of view Intermediate stage in southern border schools and its relationship to some variables
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The aim of the current research is to know the degree to which middle school teachers and female teachers in the southern border schools use electronic educational alternatives in the field of education from their point of view and its relationship to some variables, and to achieve this goal, a random sample of (200) teachers was selected in southern border schools, and a questionnaire was prepared to collect The data, as well as the descriptive approach was used to achieve this goal. T-test and analysis of variance were used for the statistical treatment. The results concluded that the educational courses provided to male and female teachers are not sufficient. It has also been concluded that the use of electronic educational alternativ

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Publication Date
Tue Oct 20 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Biological Activity of Complexes of Some Amino Acid
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Biological Activity of Complexes of Some Amino Acid

Publication Date
Wed Nov 01 2023
Journal Name
Ecological Engineering & Environmental Technology
Synthesis of Mn-Co-Ni Composite Electrode by Anodic and Cathodic Electrodeposition for Indirect Electro-oxidation of Phenol – Optimization of the Removal by Response Surface Methodology
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In the present work, Response Surface Methodology (RSM) was utilized to optimize process variables and find the best circumstances for indirect electrochemical oxidation of mimicked wastewater to remove phenol contaminants using prepared ternary composite electrode. The electrodeposition process is used for the synthesis of a ternary composite electrode of Mn, Co, and Ni oxides. The selected concentrations of metal salts of these elements were 0.05, 0.1, and 1.5 M, with constant molar ratio, current density, and electrolysis time of 1:1:1, 25 mA/cm2, and 2 h. Interestedly, the gathered Mn-Co-Ni oxides were deposited at both the anode and cathode. X-ray diffraction (XRD) and scanning electron microscopy (SEM) facilitated the qualitative char

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Publication Date
Thu Sep 01 2022
Journal Name
Neuroquantology
Evaluation of using of square flap in treatment of Postburn Contracture
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Background: One of the most common problems that encountered is postburn contracture which has both functional and aesthetic impact on the patients. Various surgical methods had being proposed to treat such problem. Aim: To evaluate the effectiveness of square flap in management of postburn contracture in several part of the body. Patients and methods: From April 2019 to June 2020 a total number of 20 patients who had postburn contracture in various parts of their body were subjected to scar contracture release using square flap. The follow up period was ranging between 6 months to 12 months. Results: All of our patients had achieved complete release of their band with maximum postoperative motion together with accepted aesthetic outcome. A

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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
Evaluation of the thermal conductivity of middle part of Iraqi soil
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Thermal properties of soils are important in buried structures contact problems. Although laboratory is distinctly advantageous in measuring the thermal conductivity of soil under ideal condition, given the ability to simulate relatively large-scale in place of soil bed, the field thermal conductivity of soil is not yet commonly used in many types of research. The use of only a laboratory experiment to estimate thermal conductivity may be the key reason for overestimation or underestimation it. In this paper, an intensive site investigation including field thermal conductivity tests for six different subsoil strata were performed using a thermal probe method (TLS-100) to systematically understanding the effects of field dry density, water c

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Publication Date
Sun May 10 2015
Journal Name
Al-academy
The system and Disorder of shape and content in Interior Design Educational halls in the Ministry of Labor and Social Affairs (Analytical study): رجاء سعدي لفتة
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Dealing with this study to find a link principle in the construction of the system and disorder to the promise of the principles and concepts of intellectual and philosophical form and content in the act of interior design of the halls education in the Ministry of Labor and Social Affairs , which leads to a reaction design objective and functionally and to increase the strength of the effect on users of the coaches and trainers . As it informs the side cognitive and developmental study of the design of the interior spaces . So it was the goal of research in the detection of the nature of the system and disorder with Focus indicators and the type of regulations and privacy and what constitutes the framework of knowledge in order to explai

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