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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 Sep 25 2013
Journal Name
International Journal For Sciences And Technology
Synthesis, Characterization, And Antibacterial Activities Of Manganese (II),Cobalt(II), Copper(II) ,Iron (II), Nickel (II) And Cadmium(II) Mixed- Ligand Complexes Containing Amino Acid( L- Lysine) And 1,10-Phenanthroline
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The research includes the synthesis and identification of the mixed ligands complexes of M(II) Ions in general composition [M(Lyn)2(phen)] Where L- lysine (C6H14N2O2) commonly abbreviated (LynH) as a primary ligand and 1,10-phenanthroline(C12H8N2) commonly abbreviated as "phen," as a secondary ligand . The ligands and the metal chlorides were brought in to reaction at room temperature in ethanol as solvent. The reaction required the following molar ratio [(1:1:2) (metal): phen:2 Lyn -] with M(II) ions, were M = Mn(II),Cu(II), Ni(II), Co(II), Fe(II) and Cd(II). Our research also includes studying the bio–activity of the some complexes prepared against pathogenic bacteria Escherichia coli(-),Staphylococcus(-) , Pseudomonas (-), Bacillus (-)

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Publication Date
Thu Jan 11 2018
Journal Name
Iosr Journal Of Pharmacy And Biological Sciences
Study the effect of hot aqueous extract of beetle cocoon Larinus maculatus F. on some physiological parameters in male albino mice
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Abstract: The study aimed to investigate the effect of oral administration of hot aqueous extract of beetle cocoon Larinus maculatus Faldermann, in a two doses 50 and100mg/Kg/B.wt for 3 and 6 weeks respectively on the levels of serum glucose, weight of body, and lipid profile in male mice Mus musculus. The results revealed that there was a significant (p<0.05) decrease in serum glucose level was dose and period dependent. Weight of body also reduced significantly (p<0.05) with doses and period dependent. The lipid profile level significantly (p<0.05) decreased in dose and period’s manner in each of Total cholesterol (TC), Triglyceride (TG), High Density Lipoprotein- (HDL), Low Density Lipoprotein (LDL), and Very Low Density Lipoprotei

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Publication Date
Mon Sep 30 2019
Journal Name
College Of Islamic Sciences
Some Applied Models of Appreciation   From the Book of Almbsot Imam Muhammad bin Hassan al-Shaibani (d 189 e): - Fundamental study -
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The forensic evidence important for the sources of legislation after the book of God Almighty and the Sunnah of the purified, including what is agreed upon in the protest, which is the book and the Sunnah and consensus, and what is different in the protest, such as measurement and approval and say companions and interests sent, and that the approval of the evidence that did not agree Accordingly, the terms of the fundamentalists differed and their definition differed with the similarity between each other, and the approval in some schools is an argument is not considered as the Shaafa'is, so it may correspond to measurement with them, but the approval at the tap and those who agree is a hidden measurement is likely to clear measurement,I

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Publication Date
Mon Oct 01 2012
Journal Name
Iraqi Journal Of Physics
Study the effect of adding TiO2 nano-powder on some surface properties of TiO2 thin film prepared on stainless steel substrate
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In this research TiO2 nano-powder was prepared by a spray pyrolysis technique and then adds to the TiO2 powder with particle size (0.523 μm) in ratio (0, 5, 10, 15 at %) atomic percentage, and then deposition of the mixture on the stainless steel 316 L substrate in order to use in medical and industrial applications.
Structure properties including x-ray diffraction (XRD) and scanning electron microscope (SEM0, also some of mechanical properties and the effect of thermal annealing in different temperature have been studied. The results show that the particle size of a prepared nano-powder was 50 up to 75 nm from SEM, and the crystal structure of the powders (original and nano powder) was rutile with tetragonal cell. An improvement in

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Publication Date
Tue Jun 23 2020
Journal Name
Annal S Of Tropical Medicine & Public Health
Histological Evaluation of local application of Phyllunthus amarus extracted powder and its combination with fibronectin protein on Wound Healing of rats
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Background: A wound is defined as a break or damage in the skin, resulting from physical or thermal damage or as a result of the presence of an underlying medical or physical condition. Herbal medicine can be called one of the branches of medicine in various forms.Phyllunthus amarus is a small herb well known for its medicinal properties and widely used worldwide. P. amarus is an important plant of Indian Ayurvedic system of medicine. Fibronectin is a major component of the extracellular matrix. It is secreted by various cells, primarily fibroblasts, as a soluble protein dimer and is then assembled into an insoluble matrix in a complex cell-mediated process. Materials and methods: Forty rats will be subjected for a surgical operation

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Publication Date
Sun Jan 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
An Evaluation of Activity of Prepared Zinc Nanoparticles with Extract Green Plant in Treatments of Diclofenac, Levofloxacin, and Tetracycline in Water
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Myrtle plant was washed, dried, and powdered after harvesting to produce a fine powder used in water treatment. An alcoholic extract was created from the myrtle plant using ethanol, which was then analyzed using GC-Mass, Fourier Transform Infrared spectroscopy, and ultraviolet-visible spectroscopy to identify the active components. Zinc nanoparticles were created using alcoholic extract. FT-IR, UV-Vis, SEM, EDX, and TEM were used to characterize zinc nanoparticles. Using a continuous processing procedure, zinc nanoparticles with myrtle extract and powder were employed to clean polluted water containing pesticides and antibiotic. First, 2 g of zinc nanoparticles was mixed with 20 ml of polluted water and the result was (Tetra 44%, Levo 32%),

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of the Role of Interleukein-2 and Interleukein-4 in the Immunopathogenesis of Steroid Therapy Resistance in Iraqi Asthmatic Patients
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Interleukins (IL-2 and IL-4) are increased in asthmatics and were reported to induce resistance to steroid therapy in some patients who fail to get benefit from glucocorticoids when used in full dose and for long period of time. In this context, the present study was conducted on Iraqi patients to provide additional laboratory mean, beside the clinical diagnosis, for the decision whether the asthma is steroid sensitive or resistant by monitoring the level of immunoglobulins, complement proteins and interleukins among asthmatic patients (steroid sensitive or resistant) and the possible contribution of other factors like age, sex and environments in the development of steroid resistance. A total number of 55 asthmatics and 28 normal subjec

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Publication Date
Sat Jun 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Evaluation of the Possible Protective Effect of Fisetin against Cyclophosphamide-induced Genotoxicity in Bone Marrow and Spleen Cells of Male Rats
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Fisetin is a plant flavonoid found in strawberries and other fruits and vegetables such as apples, persimmons, and onions. It has many pharmacological effects like anti-inflammatory, antioxidant, cardioprotective, neuroprotective, and anti-carcinogenicity which are attributed to its ability to reduce oxidative stress which considers the main reason for different disease conditions. Genotoxicity refers to the genetic material destruction within the cell which can be caused by different chemicals as well as radiation. The present study evaluates the effect of orally-administered fisetin daily for seven constitutive days on genotoxicity induced by cyclophosphamide in rats’ bone marrow and spleen cells. Results showed that fisetin exh

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Publication Date
Thu Apr 12 2012
Journal Name
Pramana
Nucleon momentum distributions and elastic electron scattering form factors for some 1p-shell nuclei
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Determination Oxidant - Antioxidant Enzyme and some Trace Elements in Breast Cancer in Baghdad City
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level of effectiveness of Glutathione - S - Transferees (GST), Glutathione peroxides (GPX),Malondialdehyde (MDA) the product of lipid peroxidation and some trace elements ( zinc,seleinum,iron ,copper ) had been measured in sera of (50) women with breast disease.which had been divided to : Control group (25),The first group (A) benign breast tumors (25),the second group (B) breast cancer (25). The results showed a clear moral high level of Glutathione - S - Transferees (GST), Glutathione peroxidase (GPX) , and Malondialdehyde (MDA) level in breast cancer group while a slight increase were observed in the levels of these enzymes and(MDA) in benign breast group. A significant reduction was evident in the levels of selenium and zinc

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