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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
Mon Jul 01 2019
Journal Name
Journal Of Physics: Conference Series
Synthesis and Characterization of new Manganese(II), Cobalt(II), Cadmium(II) and Mercury(II) Complexes with ligand [N-(3-acetylphenylcarbamothioyl)-2-chloroacetamide] and their Antibacterial Studies
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Abstract<p>Addition chloro acetyl isothiocyanate (C<sub>3</sub>H<sub>2</sub>ClNOS) with 3-Aminoaceto phenone (C<sub>8</sub>H<sub>9</sub>NO) to prepare a fresh Ligand [N-(3-acetyl phenyl carbamothioyl)-2-chloroacetamide](L). The ligand (L) behaves as bidentate coordinating through O and S donor with metal ions, the general formula of all complexes [M(L)<sub>2</sub>(Cl)<sub>2</sub>](M<sup>+2</sup> = Manganese(II), Cobalt(II), Cadmium(II) and Mercury(II)). Compounds were investigation by Proton-1, Carbon -13 NMR spectra (ligand (L) only), Element Microanalysis for C, N, H, O, S, Fourier-transform infrared, UV visible, Conductance</p> ... Show More
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Publication Date
Sun Mar 01 2009
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Tripodal Tetradentate Ligand Type NS3 and its Complexes with Re(V), Ni(II), Cu(II), Zn(II), Cd(II), and Hg(II)
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This work represents the preparation of the starting material, 3-chloro-2-oxo-1,4-dithiacyclohexane (S) using a new method. This material was reacted with, 4-phenylthiosemicarbazide to give (H3NS3) as a tetradentate ligand H3L. New complex of rhenium (V) with this ligand of the formula [ReO(L)] was prepared. New complexes of the general formula [M(HL)] of this ligand when reacted with some metal ions where: M = Ni(II), Cu(II), Cd(II), Zn(II), Hg(II) have been reported. The ligand and the complexes were characterized by infrared, ultraviolet–visible, mass, 1H nuclear magnetic resonance and atomic absorption spectroscopic techniques and by (HPLC), elemental analysis, and electrical conductivity. The proposed structure for H3L with Re (V) i

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Publication Date
Mon Mar 01 2010
Journal Name
Iraqi J Pharm Sci,
Synthesis, Characterization and Antibacterial Activities of Ligand Type N2O4 Schiff base and its Novel Complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions
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The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu

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Publication Date
Wed Dec 27 2017
Journal Name
Al-khwarizmi Engineering Journal
The Determination of Critical-Sampling Scheme of Preprocessing for Multiwavelets Decomposition as 1st and 2nd Orders of Approximations.
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One of the important differences between multiwavelets and scalar wavelets is that each channel in the filter bank has a vector-valued input and a vector-valued output. A scalar-valued input signal must somehow be converted into a suitable vector-valued signal. This conversion is called preprocessing. Preprocessing is a mapping process which is done by a prefilter. A postfilter just does the opposite.

The most obvious way to get two input rows from a given signal is to repeat the signal. Two rows go into the multifilter bank. This procedure is called “Repeated Row” which introduces oversampling of the data by a factor of 2.

 For data compression, where one is trying to find compact transform representations for a

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Publication Date
Thu Dec 01 2022
Journal Name
Journal Of Ovonic Research
Study structure and optical properties of Ag2Se, Ag2Se0.8Te0.2 and Ag2Se0.8S0.2 thin films
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Silver sulfide and the thin films Ag2Se0.8Te0.2 and Ag2Se0.8S0.2 created by the thermal evaporation process on glass with a thickness of 350 nm were examined for their structural and optical properties. These films were made at a temperature of 300 K. According to the X-ray diffraction investigation, the films are polycrystalline and have an initial orthorhombic phase. Using X-ray diffraction research, the crystallization orientations of Ag2Se and Ag2Se0.8Te0.2 & Ag2Se0.8S0.2 (23.304, 49.91) were discovered (XRD). As (Ag2Se and Ag2Se0.8Te0.2 & Ag2Se0.8S0.2) absorption coefficient fell from (470-774) nm, the optical band gap increased (2.15 & 2 & 2.25eV). For instance, the characteristics of thin films made of Ag2Se0.8Te0.2 and Ag2Se0.8S0.2

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Publication Date
Fri Jun 20 1930
Journal Name
College Of Islamic Sciences
Besharat and Quranic signs of the Prophet Muhammad (PBUH): Study and analysis
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In this paper, I highlight the bishops mentioned in the Bible in its sections
(The Old and New Testaments) where these books still retain the remaining remnant of the Bible
Issuing the prophets who preceded the mission of the Prophet Muhammad (peace and blessings of Allaah be upon him) and they must pray
And peace, as those bishops were mentioned in the Book of Formation through the recitation of the psalms
To Habakkuk, Malakhi, and Hajji.
As well as in the New Testament, which we see clearly in the four Angels: Matthew, Luke,
Disco, John.
Then the male lamented what was said of those bishops by expressing the eternal heavenly book (the Qur'an)
Al - Karim) as he focuses on this subject from multiple angles and exp

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Publication Date
Wed Aug 15 2018
Journal Name
Al-khwarizmi Engineering Journal
Construction and Characterization of Organic Solar Cell and Study the Operational Properties
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This article reviews the construction of organic solar cell (OSC) and characterized their optical and electrical properties, where indium tin oxide (ITO) used as a transparent electrode, “Poly (3-hexylthiophene- 2,5-diyl) P3HT / Poly (9,9-dioctylfluorene-alt-benzothiadiazole) F8BT” as an active layer and “Poly(3,4-ethylenedioxythiophene)-poly (styrene sulfonate)” PEDOT: PSS which is referred to the hole transport layer. Spin coating technique was used to prepared polymers thin film layers under ambient atmosphere to make OSC.  The prepared samples were characterized after annealing process at (80 ͦ C) for (30 min) under non-isolated circumference. The results show a value of filling factor (FF) of (2.888), (0.233) and (0.28

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Publication Date
Sun Mar 05 2017
Journal Name
Baghdad Science Journal
The Relation between Bacterial and Heavy Metal Water Pollution and Blood Micronuclei as Biomarkers in the Tigris River Fish
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The objective of this study is to evaluate the bacterial count and heavy metal concentration of river water on fish micronuclei. Fish and water samples are carried out in 1 May to 1 June 2013 from Tigris River. A total of fifty three fish sample are studied. The bacteriological quality of water showed that the total viable count is ranged from 150×103 to 352×103 cfu/ml and fecal coliform counts was 1250 cell/100ml during the study period. All the metals (Cu, Hg, Pb, and Zn) are within the normal limit, but Cd was slightly elevated in river water samples. The appearance of micronuclei in red blood cells of all fish species is detect , by recording a larger number of it, in ( Abu Alsomere , Hishne , Bannini Kaber al fam & Karkoor

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Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
The trend to Joint Audit as an approach to Improve the Financial Reports Quality - An Applied Study –
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This study aimed at identifying the trend to applying the Joint Audit as an approach to improve the financial reports quality with all their characteristics (Relevance, Reliability, Comparability, Consistency), as well as enclose the difficulties that faced the auditors in the Gaza Strip in implementing the Joint Audit. In order to achieve the study aims, a measure was used to identify the trend to apply the Joint Audit and it was distributed to the study sample which is consisting of (119) individuals and retrieved thereof (99) valid for analysis, approximately (83.2%), (69) of them are Auditors, (30) financial managers and accountants. The researcher used the analytical descriptive method, and after analyzing the results, the s

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Publication Date
Sat Jul 01 2023
Journal Name
The Egyptian Journal Of Hospital Medicine
Evaluation of the Antibiofilm Activity of Laurus nobilis Leaves Extract and Assessment of Its Effect on fimA and papC genes in Escherichia coli isolates
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Background: The beneficial gut bacterium E. coli can cause blood poisoning, diarrhoea, and other gastrointestinal and systemic disorders. Objective: This study amid to examines the antibiofilm activity of Laurus nobilis leaves extract on E. coli isolates and compares pre- and post-treatment gene expression of fimA and papC genes. Subjects and Methods: Ten isolates of E. coli were obtained from the Genetic Engineering and Biotechnology Institute, University of Baghdad, which was previously collected from Baghdad city hospitals and diagnosed by chemical tests, the diagnosis was confirmed using VITEK-2 System. The preparation of the aqueous and methanolic Laurus nobilis leaves extracts was done by using the maceration method and Soxhlet appara

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