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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
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility
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Abstract

            Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis,  and for the prophylaxis of fungal infections in immunocompromised patients.

           The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.

          Itraconazole nanosuspension was produced by a

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Publication Date
Sat May 01 2021
Journal Name
Key Engineering Materials
Synthesis and Characterization of the Thin Films NiSe2/Si Heterojunction for Solar Cells
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Thin film solar cells are preferable to the researchers and in applications due to the minimum material usage and to the rising of their efficiencies. In particular, thin film solar cells, which are designed based one transition metal chalcogenide materials, paly an essential role in solar energy conversion market. In this paper, transition metals with chalcogenide Nickel selenide termed as (NiSe2/Si) are synthesized. To this end, polycrystalline NiSe2 thin films are deposited through the use of vacuum evaporation technique under vacuum of 2.1x10-5 mbar, which are supplied to different annealing temperatures. The results show that under an annealed temperature of 525 K,

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Publication Date
Thu May 23 2013
Journal Name
Journal Of The College Of Basic Education
Synthesis and Characterization of Benzoic Acid 2-Salicylidene Complexes with Selected Metal Ions
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Salicylaldehyde was reacting with 2-amino benzoic acid to produce the Schiff base ligand benzoic acid 2-salicylidene (L). The prepared ligand was identified by Microelemental Analysis, FT.IR and UV-Vis spectroscopic techniques. A new complexes of Co(II),Ni(II),Cu(II) and Zn(II) with Schiff base was prepared in aqueous ethanol with a (1:1) M:L. The prepared complexes were characterized using flame atomic absorption, (C.H.N) Analysis, FT.IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements. Biological activity of the ligand and complexes against three selected types of bacteria were also examined. Some of the complexes exhibit good bacterial activities. From the obtained data the tetrahedral str

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Publication Date
Sun Jun 07 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization, Thermal Analysis and Structural Studies of New Complexes with Tetradentate Ligand
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Some new complexes of 4-(5-(1,5-dimethyl-3-oxo-2-phenyl pyrazolidin-4- ylimino)-3,3-dimethyl cyclohexylideneamino) -1,5- dimethyl-2- phenyl -1H- pyrazol -3(2H) –one (L) with Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Pd(II), Re(V) and Pt(IV) were prepared. The ligand and its metal complexes were characterized by phisco- chemical spectroscopic techniques. The spectral data were suggested that the (L) as a neutral tetradentate ligand is coordinated with the metal ions through two nitrogen and two oxygen atoms. These studies revealed Octahedral geometries for all metal complexes, except square planar for Pd(II) complex. Moreover, the thermodynamic activation parameters, such as ?E*, ?H, ?S, ?G and K are calculated from the TGA curves using Coa

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Publication Date
Wed Mar 25 2015
Journal Name
Comptes Rendus Chimie
A novel method for the synthesis of biodiesel from soybean oil and urea
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The increasing demand for energy has encouraged the development of renewable resources and environmentally benign fuel such as biodiesel. In this study, ethyl fatty esters (EFEs), a major component of biodiesel fuel, were synthesized from soybean oil using sodium ethoxide as a catalyst. By-products were glycerol and difatty acyl urea (DFAU), which has biological characteristics, as antibiotics and antifungal medications. Both EFEs and DFAU have been characterized using Fourier transform infrared (FTIR) spectroscopy, and 1H nuclear magnetic resonance (NMR) technique. The optimum conditions were studied as a function of reaction time, reactant molar ratios, catalyst percentage and the effect of organic solvents. The conversion ratio of soybea

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Publication Date
Tue Dec 05 2023
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Properties of Trimethylolpropane Triesters from Coconut (Cocos nucifera) Methyl Esters
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In this study, the acid-alkaline transesterification of refined coconut seed oil (RCOSO) to fatty acid methyl ester was followed by the production of a trimethylolpropane-based thermosensitive biolubricant using potassium hydroxide, and its physicochemical characteristics were evaluated. The American Standard Test for Materials (ASTM) was employed to ascertain the biolubricant's pour point and index of viscosity, which were found to be -4 oC and 283.75, respectively. The opposite connection between lubricant viscosity and temperature was shown by the measured viscosities at varied transesterification to be transformed into biodiesel. Following this, a biolubricant was created by further transesterifiedtemperature. The ester gr

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Publication Date
Sat Mar 28 2015
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of 5-amino-1,3,4-oxadiazole Derivitives Containing 2,6-dimethoxyphenol
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4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid was synthesized from multisteps and converted to their corresponding hydrazide. The corresponding hydrazide was cyclized to their corresponding 5-amino-1,3,4-oxadizole. Newly Schiff bases (7a-7e) were synthesized from reaction the 5-amino-1,3,4-oxadizole with several substituted of 4-hydroxybenzylaldehyde. The resulting compounds were characterized based on their IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to test the antioxidant properties of the synthesized compounds. Compound 7d and 7e exhibited significant free-radical scavenging ability in both assays.

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Synthesis and Characterization of 2-(2-hydroxy-phenyl)-3-(-R- benzothiazol-2-yl)
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were prepared by condensation of 6-R-2amino bcnzothiazol with Salicyldehyde.These Schiff bases were found to reach with maleic anhydride and citraconic to give

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Publication Date
Mon Oct 16 2006
Journal Name
No Journal
Novel Metal Complexes of Tetradentate Ligands Type N2S2 Synthesis and Physico-Chemical Characterisation
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This study is included the preparation of two tetradentate amide-thiol proligands of the general structure [H2Ln], [where; (n = (1–2)]. The ligands [H2L1] and [H2L2] have been prepared from the reaction of the cyclic thioester 2-oxo-1, 4-dithiacyclohexane (compound 1) and 3-chloro-2-oxo-1, 4 dithiacyclohexane (compound 2) with 2-aminomethanepyridine in (1:1) ratio respetively. The reaction was carried out in chloroform at room temperature and under N2 atmosphere. Structural formula of these two ligands have been reported.

Publication Date
Mon Mar 22 2010
Journal Name
Al- Mustansiriya J. Sci
Synthesis of New Amides and Schiff Bases derived From 2-Amino-1,3,4- Oxadiazole
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New compounds of amids [IV]a-e and Schiff bases [V]f-h derived from 2-amino-1,3,4-oxadiazoles [III] were synthesized and characterized by physical and spectraldata.2-Aamino-1,3,4-oxadiazoles was prepared by the action of bromine on acorresponding semicarbazide [II]( which was prepared by reaction of dialdehyde [I]with semicarbazide hydrochloride ) in the presence of sodium acetate , followed byan intramolecular cyclization . (PDF) Synthesis of New Amides and Schiff Bases derived From 2-Amino -1,3,4- Oxadiazole. Available from: https://www.researchgate.net/publication/326679206_Synthesis_of_New_Amides_and_Schiff_Bases_derived_From_2-Amino_-134-_Oxadiazole [accessed Nov 15 2023].