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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
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Molecular detection by some virulence genes of Salmonella enterica subsp. enterica isolated from the stool of children with diarrhea
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Diarrhea is a real disease in childhood which could cause death. Therefore, this study was conducted to isolate Salmonella from 350 stool samples taken from children under five years in age, suffering from diarrhea during the period from March 2019 to March 2020 in Tikrit city / Iraq. The results showed the possibility to isolate ten isolates of Salmonella enterica subsp. Enterica, an infection rate, represents 2.875% of the total rate of patients who suffer from diarrhea. The virulence genes were investigated for ten isolates of S. enterica subsp. enterica, the result is that all isolates possessed the genes stn, invA, lpfA with an appearance percentage of 100%, whi

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Publication Date
Sat Jun 01 2024
Journal Name
Journal Of Research In Dental And Maxillofacial Sciences
Relationship between Third Molar Impaction and Extraction, and Awareness about the Associated Potential Risks
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Publication Date
Fri Dec 23 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Aspirin Derivatives Exploration: A Review on Comparison Study with Parent Drug
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In recent decades, drug modification is no longer unusual in the pharmaceutical world as living things are evolving in response to environmental changes. A non-steroidal anti-inflammatory drug (NSAID) such as aspirin is a common over-the-counter drug that can be purchased without medical prescription. Aspirin can inhibit the synthesis of prostaglandin by blocking the cyclooxygenase (COX) which contributes to its properties such as anti-inflammatory, antipyretic, antiplatelet and etc. It is also being considered as a chemopreventive agent due to its antithrombotic actions through the COX’s inhibition. However, the prolonged use of aspirin can cause heartburn, ulceration, and gastro-toxicity in children and adults. This review article hi

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Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis and Identification of New 2-Substituted-1,3,4-Oxadiazole Compounds from Creatinine and Study Their Antioxidant Activities
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Publication Date
Thu Jan 01 2015
Journal Name
Ibn Al-haitham J. For Pure & Appl. Sci.
Synthesis and Characterization of Some Metal Complexes of [N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol- 4-ylcarbamothioyl) acetamide]
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A new ligand [N- (1,5- dimethyl -3- oxo- 2 – phenyl - 2 ,3 – dihydro -1H- pyrazol -4- ylcarbamothioyl) acetamide] (AAD) was synthesized by reaction of acetyl isothiocyanate with 4-aminoantipyrine, The ligand was characterized by micro elemental analysis C.H.N.S., FT-IR ,UV-Vis and 1H-13CNMR spectra, some transition metals complex of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were [M(AAD)2(H2O)2]Cl2 (M+2 = Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral.

Publication Date
Sun Mar 01 2009
Journal Name
Baghdad Science Journal
Synthesis of Some New 1,2,4-Triazoles Derived from 2-Mercaptobenzimidazole
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New 1,2,4-triazole derivatives of 2-mercaptobenzimidazole (MB) are reported. Ethyl (benzimidazole-2-yl thio) acetate (1) has been prepared by condensing 2-mercaptobenzimidazole with ethylchloroacetate. The ester (1) on reacting with hydrazine hydrate gave the corresponding acetohydrazide(2)which was reacted separately with phenylisocyanate and phenylisothiocyanate, followed by ring closure in an alkaline medium giving 3-[(benzimidazole-2-yl thio) methyl]-4-phenyl-1,2,4-triazole-5-ol and 3-[(benzimidazole-2-yl thio) methyl]-4-phenyl-1,2,4-triazole-5-thiol respectively (6,7). Reaction of acetohydrazide (2) with CS2 and ethanol/KOH, gave dithiocarbazate salt (8). Cyclization of (8) with hydrazine hydrate gave 3-[(benzimi

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Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis of Some Heterocyclic Compounds Derived from 2-Mercapto Benzoxazole
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New series of 2-mecapto benzoxazole derivatives (1-20) incorporated into fused to different nitrogen and suphur containing heterocyclic were prepared from 2-meracpto benzoxazole, when treated with hydrazine hydrate to afford 2-hydrazino benzoxazol (1). Compound (1) converted to a variety of pyridazinone andphthalazinone derivatives (2-4) by reaction with different carboxylic anhydride. Also, reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-phenyl-1,3-thiazolidin-2,4-dione-2-(benzoxazole-2-yl-hydrazone) (6). Azomethines (7-10) were prepared through reaction of (1) with aromatic aldehyde, then (7, 8) converted to thaizolidinone derivatives (11, 12). Treatment of (1) with active methylene compounds afforded deriva

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Publication Date
Thu Jun 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
Antibacterial and cytotoxic effect of a novel bio-logical Nano-silver fluoride synthesized from moringa oleifera leaf extract
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Background: A great dental and biomedical interest had been paid to silver nanoparticles because of their antimicrobial activity. Objective: To evaluate the antimicrobial and cytotoxic activity of a newly developed Nano-silver fluoride that was synthesized from moringa oleifera leaf extract against S. mutants.  Material and method: The green synthesis method was used to prepare Nano-silver fluoride from moringa oleifera leaf extract. The minimum inhibitory concentration and the minimum bactericidal concentration were evaluated using brain heart infusion plates, while the cytotoxicity was evaluated by the hemolytic activity. Results: Nano-silver fluoride had a bactericidal and bacteriostatic effect (MIC was 60 ppm a

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Publication Date
Sat Nov 10 2018
Journal Name
Oriental Journal Of Chemistry
New Series of Substituted Heterocyclics Derived from α , β – Unsaturated Ketone and Their Cytotoxic Activity Tumor Cell Lines
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The aldol condensation of 2-acetylnaphthalene with 9-anthracene carboxaldehyde afforded α, β-unsaturated keton (1) . New heterocyclic compounds containing: cyclohexenone[2], indazole[3], pyrimidinethion [4], thiazolo fused pyrimidine[5], isoxazoline[6], substituted pyrazoline[7]a-d and pyrimidinone[8] rings system were synthesized from α, β-unsaturated keton[1]. Cyclization of [1] with ethylacetoacetate gave the mentioned heterocycle cyclohexanone [2]. The cyclo condensation of [2] with hydrazine gave the new indazole derivative [3]. furthermore, the reation of [1]with thiourea gives thiopyrmidine derivative [4]. The cyclo condensation of [4] with chloroacetic acid gave the fused rings [5]. Then reacted compound[1] with hydroxy

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Publication Date
Thu Oct 08 2015
Journal Name
Journal Of Kerbala University
Synthesis, Spectroscopic and Biological Studies of some metal ions complexes with 1-Phenyl-3-pyridin-2-ylmethyl-thiourea
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حضر الليكاند (L) 1-فنيل-3-بردين-2-يل مثيل-ثايويوريا من تفاعل 2-أمينو مثيل بردين مع فنيل ايزوثايوسيانيت وبنسبة 1: 1 وشخص الليكاند بواسطة التحليل الدقيق للعناصر (C, H, N), الأشعة تحت الحمراء، الأشعة فوق البنفسجية–المرئية وطيف الرنين النووي المغناطيسي كما حضرت وشخصت معقدات أملاح بعض ايونات العناصر الثنائية التكافؤ (Co, Ni, Cu, Cd and Hg). استخدمت تقنية الأشعة تحت الحمراء، الأشعه فوق البنفسجية-المرئية, التوصيلية الكهربائية و الا

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