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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
Fri Jan 01 2021
Journal Name
Annals Of The Romanian Society For Cell Biology
Molecular study to the fungus Neosetophomasamarorum was isolated from Al Chabaish marsh, South of Iraq
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IA Ali, FK Emran, DF Salloom, Annals of the Romanian Society for Cell Biology, 2021

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Publication Date
Thu Aug 13 2020
Journal Name
Asia Pacific Journal Of Molecular Biology And Biotechnology
The anticancer molecular mechanism of Carnosol in human cervical cancer cells: An in vitro study
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Carnosol, a phenolic diterpene, is one of the effective anticancer agents naturally occurring in rosemary, sage, parsley, and oregano. The chemoresistance problem increased with the routinely used chemotherapy. Therefore, the efforts to find a substitute with safe and low cost have become crucial worldwide. The current study attempts to inspect the anticancer molecular mechanisms of Carnosol on modulating up- and down- regulation of multiple genetic carcinogenesis pathways. The cytotoxicity of Carnosol on Hela cells was evaluated by MTS assay. Flow cytometry was used to assess apoptosis and cell cycle arrest. The apoptotic morphological changes were obvious by dual apoptosis assay. The differential gene expression after treatment wi

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
PREPARATION OF NITRATION DERIVATIVES OF BILE SALTS AND ACIDS FOR MEDICAL USE
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The derivatives formed after the successive acetylation, esterification and nitration reactions to cholic, deoxycholic, and taurocholic acids were identified to be of the following general strucure: Colt, Where RI=NO3, OH, 0=, or CH3COO. R2=H, NO3, OH, 0-=, or CH3COO. R3=H, NO3,01-1, 0=, or CH3COO. R4=OH, NH(CH2)2S03Na, NH(CH2)2S03H, or OMe. By using U.V-visible and I.R spectrophotometry . The number of hydroxyl groups was determined, purity was checked from T.L.C, Most of these derivatives will find pharmaceutical application.

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Publication Date
Thu Oct 20 2022
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Study the Efficiency of Poly Nicotine Amide as Anticorrosion Coating on Stainless Steel and Study Its Biological Activity
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Using an electrochemical polymerization technique at room temperature, poly nicotine amide (PNA) was produced from the monomer nicotine amide (NA) in aqueous solution. The structure of polymer layer generated on the stainless steel surface (316 L) (working electrode) is investigated by Fourier Transmission Infrared Region (FT-IR). The anti-corrosion activity of polymer coating on the stainless steel (SS 316 L) is investigated by electrochemical polarization in 0.20M solution of HCl at 293-323K. The graphene -modified polymer film-coated SS had greater protection efficiency (PE percent) when compared to Nano ZnO -modified polymer film-coated SS. For the corrosion process of SS 316 L, kinetic and thermo-dynamic parameters of activatio

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Publication Date
Wed Mar 23 2022
Journal Name
Journal Of Educational And Psychological Researches
The level of evaluation of the educational counselors ’performance as a predictor of their level of satisfaction with their evaluation
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The current research aims to reveal the level of satisfaction of the mentors with the evaluation of their performance according to gender (male - female) and to formulate the predictive equation for the level of performance (dependent variable) from knowing the level of satisfaction with the evaluation (independent variable). (16 paragraphs) contains alternatives to the answer that measures the level of satisfaction (weak, medium, and high) (1,2,3), that is, with a hypothetical average of (32). It consisted of 100 educational counselors consisting of 45 males and 55 females, the results of the research concluded that the level of satisfaction with performance is below the mean when compared with the hypothetical average of the scale of s

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Publication Date
Sun Sep 03 2017
Journal Name
Baghdad Science Journal
Evaluation of bioactivity against some pathogenic bacteria and oxidation for fungal secondary metabolites of Fusarium solani isolated from soil
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The study included isolate and diagnose fungus Fusarium solani of the local soil and purified and development in the PDB medium and the filtrate extracted using a solvent (Ethyl acetate) to obtain the fungal secondary metabolites extract. This extract has shown bioactivity against both reference isolates (E.coli (ATCC25922) and S.aureus(NCTC6571)) and pathogenic isolates S.pyogenes, K. pneumonia and S.typhimurium using agar disk diffusion technique , The diameters of the inhibition zones of fungal secondary metabolites24.0 mm against E.coli and 31.5 mm against S.aureus,and 34.0 mm against K.pneumoniae and 18.0 mm against S.pyogenes and 33.5mm against S.typhimurium. The test revealed the minimum inhibitory concentration (MIC) of the fungal

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Publication Date
Fri Jan 13 2023
Journal Name
World Academy Of Sciences Journal
Potential effects of miR‑146 expression in relation to malondialdehyde as a biomarker for oxidative damage in patients with breast cancer
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Publication Date
Fri Oct 26 2018
Journal Name
Journal Of Planner And Development
Acceptable and Unacceptable Growth of Industrial Agglomeration in Urban Environment. Baghdad as Case Study
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Publication Date
Mon Oct 01 2012
Journal Name
Iraqi Journal Of Physics
Comparison study of some mechanical properties of micro and nano silica EP composites
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The effect of micro-and nano silica particles (silica SiO2 (100 μm), Fused silica (12nm)) on some mechanical properties of epoxy resin was investigated (Young's modulus, Flexural strength). The micro-and nano composites were prepared by using three steps process with different volume fraction of micro-and nano particles (1, 2, 3, 4, 5, 7, 10, 15, and 20 vol. %). Flexural strength and Young's modulus of nano composites were increased at low volume fraction (max. enhancement at 4 vol.% ). However at higher volume fraction both Young's modulus and flexural strength decrease. Moreover, above, the mechanical properties are enhanced more than that of neat epoxy resin. The flexural strength decreases with increasing the volume fraction of micr

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Publication Date
Mon Dec 18 2017
Journal Name
Agronomy
A Case Study of Potential Reasons of Increased Soil Phosphorus Levels in the Northeast United States
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Recent phosphorus (P) pollution in the United States, mainly in Maine, has raised some severe concerns over the use of P fertilizer application rates in agriculture. Phosphorus is the second most limiting nutrient after nitrogen and has damaging impacts on crop yield if found to be deficient. Therefore, farmers tend to apply more P than is required to satisfy any P loss after its application at planting. Several important questions were raised in this study to improve P efficiency and reduce its pollution. The objective of this study was to find potential reasons for P pollution in water bodies despite a decrease in potato acreage. Historically, the potato was found to be responsible for P water contamination due to its high P sensitivity a

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