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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
Wed Oct 02 2019
Journal Name
Biochem. Cell. Arch.
NEW MIXED LIGAND OF DITHIOCARBAMATE AND 8- HYDROXYQUINOLINE WITH SOME COMPLEXES OF SCHIFF BASE LIGAND : SYNTHESIS, SPECTRAL ANALYSIS AND BIOLOGICAL ACTIVITY
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The preparation, spectroscopic characterisation of complexes derived from the mixed ligands with CdII, ZnII and CoII metal ions with Schiff base, Dithiocarbamates (DTCs) and 8-Hydroxyquinoline are reported. The compounds that prepared have been defined via; chloride content, F.T-IR, UV-Vis 1H-NMR spectroscopy and C.H.N.S, as well as conductance and magnetic susceptibility.All data which collected from such methods specified complexes with 6 coordinates in solution and solid states. The biologicalactivity that is related to all the prepared compounds which were screened for their antimicrobial activitiesagainst (G+ and (G- )). The data that collected from biological activity indicate that complexes will have extra activity against such teste

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Publication Date
Sun Oct 20 2019
Journal Name
Biochemical And Cellular Archives
NEW MIXED LIGAND OF DITHIOCARBAMATE AND 8- HYDROXYQUINOLINE WITH SOME COMPLEXES OF SCHIFF BASE LIGAND : SYNTHESIS, SPECTRAL ANALYSIS AND BIOLOGICAL ACTIVITY
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The preparation, spectroscopic characterisation of complexes derived from the mixed ligands with CdII, ZnII and CoII metal ions with Schiff base, Dithiocarbamates (DTCs) and 8-Hydroxyquinoline are reported. The compounds that prepared have been defined via; chloride content, F.T-IR, UV-Vis 1H-NMR spectroscopy and C.H.N.S, as well as conductance and magnetic susceptibility.All data which collected from such methods specified complexes with 6 coordinates in solution and solid states. The biologicalactivity that is related to all the prepared compounds which were screened for their antimicrobial activitiesagainst (G+ and (G-)). The data that collected from biological activity indicate that complexes will have extra activity against such tested

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Publication Date
Thu Aug 31 2017
Journal Name
Available At Ssrn 3030385
Synthesis, Spectral Studies And Antimicrobial Activity Of Mixed Ligand Complexes Of Cephalexin And Dimethylglyoxime With Some First Row Transition Metal Ions
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In this paper ,six new mixed metal ligand complexes are reported with Cephalexin (Ceph.H)as a primary ligand and Dimethylglyoxime (DMG) as secondary ligand with metal Chloride [MCl2 .nH2O. M=Mn(II),Co(II),Cu(II),Ni(II) and Zn(II),n=0-6] ,CrCl3.6H2O.The complexes are of (1:1:1)(Metal:Ligand: Ligand) Stoichiometry.The structures of these complexes are confirmed by using FT-IR and UV- electronic spectroscopies, magnetic moments, melting points, molar conductivity measurements and the metal % analysis revealed that the complexes analyze indicates a four coordinated as (A)=[M(HDMG) (Ceph)] .M=[Ni(II)and Zn(II).Six coordinated as (B) = K2[M(DMG)(CePh)(H2O)]. M= Mn (II),Co(II) and Cu(II) and (C)=[Cr(DMG)(Ceph)]Cl2. Interestingly, the in-vitro anti

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Publication Date
Fri Feb 15 2019
Journal Name
Research Journal Of Pharmaceutical, Biological And Chemical Sciences
Synthesis, Spectroscopic, Characterization and Biological Activities of Schiff Base Ligand and Metal Complexes of Some Metal (II) Salts with Anthranilic Acid
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Schiff base N,N'-Bis-(4-dimethylamino-benzylidene)-benzene-1,4-diamine has been synthesized from 4-dimethylaminobenzenaldehyde and benzene-1,4-diamine. The structure of Schiff base was obtained by (C.H.N.) microanalysis, Mass, 1HNMR, FT-IR and UV-Vis spectral methods and thermal analysis. Metal mixed ligand complexes of some metal(II) salts with Schiff base ligand and anthranilic acid were prepared in the molar ratio (1:2:2), (Metal):(SBL)2:(Anthra)2, (SBL)= Schiff base ligand, (Anthra) =anthranilic acid and Metal= Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II). The thermal behaviour (TGA) of the complexes was studied. The prepared complexes identified by using mass, thermal analysis, FT.IR and UV-Vis spectrum methods, on otherwise flame

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Publication Date
Wed Jun 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
Potential of Salivary Matrix Metalloproteinase 9 to Discriminate Periodontal health and disease
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Periodontitis is a chronic inflammatory disease resulted from aggravated immune response to a dysbiotic subgingival microbiota of a susceptible host. Consequences of periodontitis are not only limited to the devastating effect on the oral cavity but extends to affect general health of the individual and also exerts economic burdens on the health systems worldwide. Despite these serious outcomes of periodontitis; however, they are avoidable by early diagnosis with proper preventive measures or non-invasive interventions at earlier stages of the disease. Clinically, diagnosis of periodontitis could be overlooked due to certain limitations of the conventional diagnostic methods such as periodontal charting and radiographs. Utilization of re

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Publication Date
Sat Apr 01 2023
Journal Name
Science Of The Total Environment
Recent advances and applicable flexibility potential of electrochemical processes for wastewater treatment
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This study examined >140 relevant publications from the last few years (2018–2021). In this study, classification was reviewed depending on the operation's progress. Electrocoagulation (EC), electrooxidation (EO), electroflotation (EF), electrodialysis (ED), and electro-Fenton (EFN) processes have received considerable attention. The type of action (individual or hybrid) for each electrochemical procedure was evaluated, and statistical analysis was performed to compare them as a new manner of reviewing cited papers providing a massive amount of information efficiently to the readers. Individual or hybrid operation progress of the electrochemical techniques is critical issues. Their design, operation, and maintenance costs vary depending o

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Publication Date
Sun Sep 01 2019
Journal Name
Journal Of Physics: Conference Series
Evaluation of Nuclear safety procedures in some Iraqi universities
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Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Antibacterial of 2,3-Dihydrobenzo Thiazole-2-Carboxylic Acid Complexes with Some Selected Metal Ions
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A new ligand 2,3-dihydrobenzo [d] thiazole-2-carboxylic acid (L) has been prepared from the reaction of ortho amino phenyl thiol with dichloroacetic acid in mole ratio (1:1). It has been characterized by elemental analysis (C.H.N.), IR, UV- Vis.spectraand 1H, 13C-NMR. A new series complexes of the bivalent ions (Co, Ni, Cu, Pd, Cd, Hg and Pb) and the trivalent (Cr) have been prepared and characterized too. The structural has been established by elemental analysis (C.H.N.), IR, UV-Vis. spectra, molar conductivity, atomic absorption and magnetic susceptibility measurements. The synthesized complexes were prepared in (1:2) ratio correspond to (Co(II), Ni(II), Cu(II), Pd(II), Cd(II), Hg(II) and Pb(II) complexes while in case Cr(III) complex is

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Publication Date
Tue Feb 04 2014
Journal Name
Al-mustansiriyah
Synthesis, Spectroscopic and Biological Studies of some Metal Complexes with 2, 4-dinitro-2-amino hydrozo benzene.
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Publication Date
Tue Jul 31 2012
Journal Name
Journal Of The College Of Education - University Of Tikrit
Synthesis, Spectroscopic and Biological Studies of some Metal Complexes with 1-phenyl-2(1-phenyl ethylidene) hydrozine.
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