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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
Tue May 13 2014
Journal Name
International Journal Of Chemical And Process Engineering Research
SYNTHESIS, PHYSICO-CHEMICAL AND ANTIMICROBIAL PROPERTIES OF SOME METAL (II) -MIXED LIGAND COMPLEXES OF TRIDENTATE SCHIFF BASE DERIVES FROM Β-LACTAM ANTIBIOTIC {(CEPHALEXIN MONO HYDRATE)-4-CHLOROBENZOPHENONE} AND SACCHARIN
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A new Schiff base (4-chlorophenyl)(phenyl methanimine (6R,7R)-3-methyl-8-oxo-7-(2-phenylpropanamido)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate=HL=C29H24ClN3O4S) has been synthesized from β-lactam antibiotic (cephalexin mono hydrate (CephH)=(C16H19N3O5S.H2O) and 4- chlorobenzophenone. Metal mixed ligand complexes of the Schiff base were prepared from chloride salt of Fe(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), in 50% (v/v) ethanol – water medium in aqueous ethanol(1:1) and Saccharin(C7H5NO3S) containing sodium hydroxide. Several physical tools in particular; IR, C:H:N , 1H NMR,13C NMR for ligand, melting point, molar conductance, magnetic moment. and determination of the percentage of the metal in the complexes by flame(AAS

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Publication Date
Sat Nov 29 2025
Journal Name
Journal Of Physical Education
Specifying Standard Scores and Levels for Some Physical Variables as Indicators for Selecting Youth Soccer Players Aged (17 – 19) years Old
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Publication Date
Wed May 01 2013
Journal Name
Chemical And Process Engineering Research
Synthesis and Characterization of Polycyclicacetal Derived from PEG & Erythro-Ascorbic Acid Derivative and Study Its Effect on the Activity of ACh Enzyme (In Vitro)
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Polycyclicacetal was prepared from the reaction of PEG with aldehyde derived from Erythro-ascorbic acid (pentulosono-ɣ-lactone-2,3-enedianisoate).All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR, and mass spectra.The inhibitory effect of prepared polymer on the activity of human serum AcetylCholinesterase has been studied in vitro. The polymer showed a remarkable activity at low concentration (4.7x10-3 – 4.7x10-8M).

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Publication Date
Thu Feb 25 2021
Journal Name
Iraqi Journal Of Agricultural Sciences
ROSEMARY VOLATILE OIL AS A PRESERVATIVE AGENT IN SOME CANNED MEAT FOODS
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This research was aimed to evaluate activity of Rosemary volatile oil and Nisin A in vivo and on B. cereus isolated from some canned meat products in vitro. The results showed that the activity of Rosemary volatile oil (2000 µg/ml) and Nisin A (350 µg\ml) attained to 27 and 19 mm inhibitory zone diameter respectively in well diffusion method. The viable plate count from samples of canned meat treated with effective concentration of Rosemary volatile oil and Nisin A were examined. The samples with Rosemary volatile oil was not showed any CFU/g after 9 days of preservation while sample with Nisin A and control observed 49 and 45 CFU/g respectively. In vivo experiment on mice, two weeks after oral dose of Rosemary volatile oil (2000

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Evaluation of Physical and, Rheological Properties of Clotrimazole Emulgel
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         Recently, emulgel has emerged as one of the most interesting topical preparations in the field of pharmaceutics. In this research clotrimazole was formulated as topically applied emulgel ; different formulas were prepared. The prepared emulgels were evaluated for their physical appearance , rheological behaviour , and in vitro drug release . The influence of the type of gelling agent (carbopol 934 and methyl cellulose), the concentration of both the emulsifying agent (2% and 4% w/w of mixture of span 20 and tween 20) and the oil phase (5% and 7.5% w/w of liquid paraffin) and the type of oil phase (liquid paraffin and cetyl alcohol), on the drug release from the prepared emulgels was invest

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Publication Date
Mon Mar 02 2015
Journal Name
Chemistry And Materials Research
Synthesis and Characterization of 3,5-Dimethyl-2- (4-nitrophenyl azo)-PhenolComplexes with Co(II) and Ni(II) and Study Its Effect on the Activity of AchEnzyme(invitro)
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Transition metal complexes of Co(II) and Ni(II) with azo dye 3,5-dimethyl-2-(4-nitrophenylazo)-phenol derived from 4-nitoaniline and3,5-dimethylphenol were synthesized. Characterization of these compounds has been done on the basis of elemental analysis,electronic data, FT-IR,UV-Vis and 1 HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of thecomplexes formed were studies following the mole ratio and continuous variation methods, Beer ' s law obeyed over a concentrationrange (1x10 -4 - 3x10 -4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, thestoichiomerty of the complexes has been found to be 1:2 (Metal:ligand). On the basis of physicochemical data tetrahedral

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Publication Date
Wed Nov 01 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Serum Soluble Angiotensin-Converting Enzyme-2 Level and Its Potential Association With The Renin-Angiotensin-Aldosterone System in Non-Hypertensive Iraqi COVID-19 Patients: An Observational Study
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Background: The novel coronavirus disease (COVID-19) is caused by Severe acute respiratory syndrome coronavirus 2 (SARS-Cov2) which utilizes angiotensin converting enzyme2 (ACE2) to invade the host cells. This membrane-bound peptidase is widely distributed in the body; its activity antagonizes the renin-angiotensin-aldosterone system (RAAS). Once SARS-Cov2 enters the cell, it causes downregulation of ACE2, resulting in the unopposed activation of RAAS. The unregulated activity of the RAAS system can deteriorate the prognosis in COVID-19 patients. A soluble form of ACE2 (sACE2) was reported to have a role in the SARS-Cov2 invasion of the susceptible cells.

Aim of the study: This study aims to inve

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Publication Date
Mon Jan 01 2001
Journal Name
University Of Jordan
A Study of Some Generalizations of Proper Mappings
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Publication Date
Mon Sep 25 2023
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, Biological Activity and Thermal Study of New Complexes [Ni II, Hg II and La III] from Mixed Ligands (Curcumin and Azo compounds type N2O2)
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The compound [L] was produced in the current study through the reaction of 4-aminoacetophenon with 4-methoxyaniline in the cold, concentrated HCl with 10% NaNO2. Curcumin, several transition metal complexes (Ni (II), La (III), and Hg (II)), and compound [L] were combined in EtOH to create new complexes. UV-vis spectroscopy, FTIR, AA, TGA-DSC, conductivity, chloride content, and elemental analysis (CHNS) were used to describe the structure of produced complexes. Biological activities against fungi, S. aureus (G+), Pseudomonas (G-), E. coli (G-), and Proteus (G-) were demonstrated using complexes. Depending on the outcomes of the aforementioned methods, octahedral formulas were given as the geometrical structures for each created comp

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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and study the liquid crystalline properties of new compounds containing 5-methyl-2,4-dihydro-3H-pyrazol-3-one
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Abstract<p>The new compounds of pyrazolines were synthesized from the reaction of different acid hydrazide with ethylacetoacetate and ethanol under reflux. These compounds were obtained from many sequence reactions. The 4-acetyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one compounds synthesized from the reaction of 5-methyl-2,4-dihydro-3H-pyrazol-3-one with acetyl chloride in calcium hydroxide and 1,4-dioxane. Finaly, Schiff bases were prepared via condensation reaction of products of mono- and tri ketone derivatives[IV]<sub>a, b</sub> with phenyl hydrazines as presented in (Scheme 1, 2). The synthesized compounds were identification by using FTIR, NMR and Mass spectroscopy (of some of them).</p> ... Show More
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