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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 May 02 2014
Journal Name
International Journal Of Scientific & Technology Research
Synthesis, Structure And Characterization Of Zns Qds And Using It In Photocatalytic Reaction
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ZnS nanoparticles were prepared by a simple microwave irradiation method under mild condition. The starting materials for the synthesis of ZnS quantum dots were zinc acetate (R & M Chemical) as zinc source, thioacetamide as a sulfur source and ethylene glycol as a solvent. All chemicals were analytical grade products and used without further purification. The quantum dots of ZnS with cubic structure were characterized by X-ray powder diffraction (XRD), the morphology of the film is seen by scanning electron microscopy (SEM). The particle size is determined by field effect scanning electron microscopy (FESEM), UV-Visible absorption spectroscopy and XRD. UV-Visible absorption spectroscopy analysis shows that the absorption peak of the as-prep

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Publication Date
Thu Dec 26 2019
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
COMPARATIVE ANATOMICAL AND HISTOLOGICAL STUDY OF SOME ORGANS IN TWO FISH SPECIES CYPRINUS CARPIO LINNAEUS, 1758 AND MESOPOTAMICHTHYS SHARPEYI (GÜNTHER, 1874)(CYPRINIFORMES, CYPRINIDAE)
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  The present study aims to give some details about the normal anatomical and histological structure of the liver, pancreas and gall bladder in Cyprinus carpio Linnaeus, 1758 and Mesopotamichthys sharpeyi (Günther, 1874). Anatomical results revealed that the liver of C. carpio is a reddish-brown in color, located in the anterior part of abdominal cavity and dispersed between most of the intestines, which is divided into two lobes; while in M. sharpeyi the liver is light brown in color located in the anterior part of abdominal cavity and extends to the end of the intestinal tract with two lobs. The gallbladder situated in the right side of the liver in both species. Histological results in both species showed that the liver consists

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Publication Date
Mon Sep 25 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Theoretical Spectroscopic Study for Some Diatomic Molecules
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      In this work, four electronic states ( ,   , and   ) of some diatomic molecules (InF and InCl) was studied by TD-DFT with energy represented by the exchange-correlation energy. The SAOP/ATZP model was applied here to determine all parameters (re, Be, De, , , Te , and were determined to creation reliable values for electron spectroscopy. Also, another set of this calculation has been used represented by two theoretical models: ATZP and et-QZ3P-xD model. Therefore these theoretical models for (   and   , and   ) of the molecules have been compared with many values, theoretical and experimental values,  and appear converge

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
A Green Synthesis of Iron/Copper Nanoparticles as a Catalytic of Fenton-like Reactions for Removal of Orange G Dye
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This research paper studies the use of an environmentally and not expensive method to degrade Orange G dye (OG) from the aqueous solution, where the extract of ficus leaves has been used to fabricate the green bimetallic iron/copper nanoparticles (G-Fe/Cu-NPs). The fabricated G‑Fe/Cu-NPs were characterized utilizing scanning electron microscopy, BET, atomic force microscopy, energy dispersive spectroscopy, Fourier-transform infrared spectroscopy and zeta potential. The rounded and shaped as like spherical nanoparticles were found for G-Fe/Cu‑NPs with the size ranged 32-59 nm and the surface area was 4.452 m2/g. Then the resultant nanoparticles were utilized as a Fenton-like oxidation catalyst. The degradation efficiency of

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Publication Date
Thu Aug 18 2022
Journal Name
Dental Hypotheses
Microleakage Evaluation of Glass Hybrid Restoration Following Usage of Papain-Based Gel and Ceramic Bur for Caries Removal: An in Vitro Study
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Publication Date
Sun Mar 01 2015
Journal Name
Baghdad Science Journal
The Effect of Age and Gender on Fetuin-A and Some Biochemical parameters in Blood Sera of Iraqi patients with T2DM: A comparative study
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The serum protein test includes measurement of the level of total protein(albumin, globulin). Fetuin-A is a blood protein made in liver. It can inhibit insulin receptor, enhance insulin sensitivity and make the individuals more likely to develop type 2 diabetes, then disorder in lipid profile (Total cholesterol(TC), low density lipoprotein cholesterol (LDL-c), high density lipoprotein cholesterol (HDL-c), Triglyceride(TG) and very low density lipoprotein cholesterol (VLDL-c) . To evaluate Fetuin-A, total protein, albumin, globulin, HbAlc and lipid profile in 200 adult and elderly Iraqi patients with type 2 Diabetes Mellitus were taken and compare them with 200 subjects as a healthy control. The laboratory analysis(for patients and

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Publication Date
Wed Mar 08 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Extraction and Estimation of β-carotene Pigment from Some Species of The Genus Rhodotorula and Study The Ability to Increas Their Production By Mutagenesis
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Beta-carotene pigment was extracted from 6 strains collected from different sources related to some species of the genus Rhodotorula sp. The maximum productivity was in the strain Rhodotorula  mucilaginosa BA61 with amount 10.25 gm/l. The minimum productivity was from the strain R. minuta BA78 with amount 5.39 gm/l. The effects of the chemical mutagen (MNNG) and the physical mutagen (UVC) on the viability of the strains was studied. The results revealed that the chemical mutagen (MNNG) with the concentration 0.2 mg/ml has the clear effect on the viability of the strains , which killing percentage reached to 65.91% in the strain R. minuta BA78. Results of the study of mutagenesis with UVC showed that increase in killing percentage fo

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Global Pharma Technology
Preparation, Characterization and Biological Activity of New Derivatives of 3-Cyclic Oxazepine, 3-Cyclic Lactam and 3- Aminomethyl Imidazo (1, 2-a) Benzthiazol
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In this work a series of fourteen new compounds were synthesized. Compound [1] was formed from the reaction of 2-aminobenzothiazole and p-bromophenacyl bromide. Aldehyde group [2] was obtained from the reaction of compound [1] with pocl3 in presence of DMF and CHCl3 .After that shiff bases have been synthesized from the reaction of compound [2] with different aromatic amine to give new shiff bases [3- 5]. These new shiff bases have been reduced to their corresponding amine [6-8] by means of sodium borohydride. Then reaction of shiff bases [3-5] with phenyl isocyanate gives 3-cyclic lactam derivatives [9-11]. 3-cyclic Oxazepine derivatives [12-14] were obtained by reaction of shiff bases [3-5] with succinic anhydride. These new formed co

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Publication Date
Mon Sep 01 2014
Journal Name
Scholars' Press
Liquid Crystals of 2,4-Substituted-1,3-Thiazole Derivatives
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A new compounds of 2,4-substituted-1,3- thiazole containing amines [I] and [II], Schiff bases [IV] and [V], amides [VI]-[X],esters [XI] - [XIII], thiazolidinones [XIV]-[XVIII] and 1,3-oxazepines [XIX]-[XXV] were Synthesized and characterized by melting points, FTIR spectroscopy, elemental analysis, 1HNMR,13CNMR, dept135and Mass spectroscopy. The liquid crystalline properties of the synthesized compounds were verified by using hot-stage polarizing optical microscopy (POM) and differential scanning calorimeter (DSC). The compound [I] was found to be nematic textures (N). The first series of this study [II]n display only enantiotropic nematic phase when n=1-5 while the compounds with n =6-8 display two mesophasese smectic C(SmC) and nematic ph

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Microbiological studies of a new naphthoquinone semicarbazone derivatives
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The antimicrobial activity of two naphthoquinone semicarbazone derivatives (Two newly synthesized compounds) have been studied by using tube — diluation and disc plate technique. The effect of those derivatives upon pathogenic microorganism iso-lated from specimen(urine iwounds,stool, swabs, throat ....etc) have been studied also in comparison with the antibiotics (amikacin,ampicillin, carbencillin, cephalothin, cefoxitin,clindamycin ,erythromycin,gentamycin,penicillin,tetracylin and tri-methoprim. It was shown that derivative(1) had more effective against micro organ-ism than derivative(11).

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