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bijps-1639
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 Jan 01 2020
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Charecterization and Antibacterial Study of New Glyoxilic Acid and Its (N2O4) MnII Ion Complex
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THE Schiff base reaction played an important role of the condensation reaction between 2-aminophenol and Glyoxylic acid in the presence of calculated amounts of KOH as a catalyst. The reaction has been carried out in ethanol under reflux and stirring condition for 3.5 hrs. All syntheses were carried out under hydrogen gas forming a new potassium (E)-1-hydroxy-2-(2-hydroxyphenylimino)ethanolate ligand type [NO2]. The ligand of the general formula K2[Mn(L2)] type and its Mnп complex K2[Mn(N2O4)] type, has been characterized by spectroscopic methods (F.T-I.R. and U.V-Vis.), elemental analysis (C.H.N) metal content, magnetic susceptibility measurement, Thin-layer chromatography (T.L.C), X-RD powder diffraction, 1H-NMR, 13C-NMR molar conductanc

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis, Characterization and study biologicalactivity of several 1-cyclopentene-1,2-dicarboxylimidyl Containing oxadiazole and Benzothiazole
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In this work involved prepared of several new 1-cyclopentene-1,2-dicarboxylimide linked to oxadiazole and benzothiazole moiety were synthesized by two steps: The first step 2-amino-substituted-1,3,4-oxadiazoles and substituted-2-aminobenzothiazole were reaction with 1-cyclopentene-1,2-dicarboxyl anhydride producing N-( 5- substituted-1,3,4-oxadiazole-2-yl)-1-cyclopentene-1,2-dicarboxyl amic acids and N-(Substitutedbenzothiazole-2-yl)-1-cyclopentene-1,2-dicarboxyl amic acids which in turn were dehydrated in the second step via fusion method to afford he desirable N-(5-substituted-1,3,4-oxadiazole-2-yl)-1-cyclopentene-1,2-dicarboxylimides and N-(Substituted benzothiazole-2-yl)1-cyclopentene-1,2-dicarboxylimides respectively. Struct

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Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Grafted Chitosan Blending with Polyvinyl alcohol / Nanocomposite and Study Biological Activity
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The study of biopolymers and their derivative materials had received a considerable degree of attention from researchers in the preparation of novel material. Biopolymers and their derivatives have a wide range of applications as a result of their bio-compatibility, bio-degradability and non-toxicity. In this paper, chitosan reacted with different aldehydes(2,4 –dichloro- benzaldehyde or 2-methyl benzaldehyde), different ketones (4-bromoacetophenone or 3-aminoacetophenone) to produce chitosan schiff base (1-4) . Chitosan schiff base (1-4) reacted with glutaric acid or adipic acid in acidic media in distilled water according to the steps of Fischer and Speier to produce compounds (5-12)

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Publication Date
Sat Dec 02 2023
Journal Name
Journal Of Engineering
Evaluation of the Stability and Flow of Asphalt Concrete Produced with Waste Brick Tile Powder as a Filler
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The utilization of recycled brick tile powder as a replacement for conventional filler in the asphalt concrete mix has been studied in this research. This research evaluates the effectiveness of recycled brick tile powder and determines its optimum replacement level. Using recycled brick tile powder is significant from an environmental standpoint as it is a waste product from construction activities. Sixteen asphalt concrete samples were produced, and eight were soaked for a day. Samples contained 5% Bitumen, 2% to 5% brick tile powder, and conventional stone dust filler. The properties of samples were evaluated using the Marshall test. It was observed that the resistance to stiffness and deformation of asphalt concrete

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Publication Date
Sun Jun 06 2010
Journal Name
Baghdad Science Journal
Synthesis of Some Heterocyclic Compounds derived from 2-mercapto pyrimidine
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In this work 2-hydrazino pyrimidine (1) was prepared from 2-mercapto pyrimidine with hydrazine hydrate. Treatment of (1) with active methylene compounds gave 2-(3,5-dimethyl -1 H – Pyrazole-1-yl) pyrimidine , whereas the reaction of (1) with carboxylic anhydride namely maleic anhydride or 1,2,3,6-tetra hydro phthalic anhydride yielded 1-Pyrimidine-2-yl-1,2-dihydro pyridazine-3,6-dione (3) and 2 – Pyrimidin -2-yl -2,3,4 a ,5,8 a – hexahydro phthalazine 1,4 – dione (4) . Reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-Phenyl-1,3-thiazolidine-2,4-dione-2( pyrimidine -2- yl hydrazone (6) Azomethine (7-10) were prepared through condensation of (1) with aromatic aldehydes or ketones, then comp

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Publication Date
Mon Aug 01 2022
Journal Name
Biochemical And Cellular Archives
EVALUATION OF THE TOXICITY OF DELTAMETHRIN INSECTICIDE ON SOME HEMATOLOGICAL PARAMETERS AND OXIDATIVE STRESS ON MICE
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Publication Date
Sun Jan 01 2023
Journal Name
8th Engineering And 2nd International Conference For College Of Engineering – University Of Baghdad: Coec8-2021 Proceedings
Potential powers of urbanism
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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Evaluation of the Epoxy/Antimony Trioxide Nanocomposites as Flame Retardant
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Publication Date
Fri Jan 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Spectroscopic, and Biological Activity Study for New Complexes of Some Metal Ions with Schiff Bases Derived From 2-Hydroxy Naphthaldehyde with 2-amine benzhydrazide
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This study describes the preparation of tetradentate Schiff base derived from the condensation of 2-Hydroxy naphthaldehyde with 2-amine benzhydrazide and the synthesis of new complexes series with a good yield.The prepared ligand was characterized using a microanalysis technique, UV-visible, FT-IR, nuclear magnetic resonance 1H-NMR, mass spectrometry, thermal gravimetric analysis TGA, and the addition of conductivity measurement and magnetic moment of complexes. The invitro antimicrobial activity of the prepared compounds was tested against  Gram-negative Klebsiella pneumonia, Gram-positive Staphylococcus aureu, and Candida albicans by the agar well diffusion method. The spectroscopy and measurement studies showed that the li

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Publication Date
Tue Mar 14 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some Mixed-Ligand Complexes Containing Azo Dye and 1,10-phenanthroline with CoII, ZnII, CdII and HgII Ions
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 In this work, the ligand was obtained from the reaction of diazonium salt of naphthyl amine with 1-amino-2-naphtol-4-sulfonic acid. The bidentate ligand  type (NO) donar atoms was reacted with 1,10-phenanthroline and matel salt in a 1:1:1 mole ratio to give the complexes, using NaOH as a base. Physical-chemical teqnichas were used to characteriz the prepared compounds FT-IR,U.V-Vis, fluorescence and 1HNMR spectroscopy, atomic absorption , chloride content along with conductivity and melting point measurements .Finally, thermal analysis was used to confirm the presence of coordination H2O molecule in the complexes structure. According to memtioned characterization methods, the general formula proposed for CoII ZnII, CdII and Hg

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