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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 Aug 06 2021
Journal Name
Research Journal Of Pharmacy And Technology
Molecular Detection and Genotyping of Human Herpes Virus 8 in a sample of Iraqi Blood Donors
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Human herpes virus-8 (HHV-8) infection has increased recently in Arabic countries. HHV-8 in healthy persons does not necessarily cause life-threatening infection, and however, it causes a more severe infection among immunocompromised patients. The distribution of HHV-8 genotypes varies according to ethnicity and depends on the geographic region prior rapid development of global travel. A cross sectional prospective study included a hundred healthy blood donor samples with a mean age of (36.60±10.381), 81% were positive for molecular detection of HHV-8 DNA. PCR results for HHV-8 were strongly related with risk factors such as the number of sexual relations, previous surgeries, blood transfusion, dental operation, and the number of b

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Publication Date
Mon Dec 28 2020
Journal Name
The Iraqi Journal Of Veterinary Medicine
Isolation and Molecular Identification of Nontuberculous Mycobacterium from Different Species of Fish in Karbala Province, Iraq
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This study was designed for isolation and molecular identification of Nontuberculous Mycobacterium (NTM) from fish during the period between October and December 2017 from Karbla province, Iraq. This study included 200 fresh fish samples from four different species including Spondyliosoma cantharus, Liza abu, Carassius carassius and Cyprinuscarpio. Three samples of each fish were taken including gills, muscles and all internal organs. The samples were processed by decontamination, concentration of 4% sodium hydroxide, and 0.1 ml of sediment was streaking on Löwenstein Johnson (LJ) media; then the bacterial cultures were incubated at 28-30 °C for 3days up to 4 weeks and suspected colonies were stained with acid fast stain to confir

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Publication Date
Sat Jun 30 2018
Journal Name
Journal Of Advanced Laboratory Research In Biology
Evaluation some Biochemical Levels in Patients undergoing Hemodialysis in Baghdad Governorate
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The objective of investigating some biochemical parameters like urea, creatinine, Hb and other parameters as CRP and leptin in the serum of ESRD patients on hemodialysis pre-dialysis. Method: Sample of 250 cases which consists of the patient with ESRD, their mean ages were 52.66 ± 12.55 years with ranged from 18-83. Moreover, under hemodialysis treatment not less than three months. Apparently, 20 healthy subjects were selected as (control) for comparison. Results: The results showed that there was a significant increase (p<0.01) in the serum urea, creatinine, CRP, and leptin. While, revealed significant (p< 0.05) decrease in the levels of uric acid, serum glucose, albumin, inorganic phosphorus, potassium, Hb and platelet in patien

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Publication Date
Sat Jun 15 2019
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the effectiveness of using platelet rich fibrin (PRF) as a sole grafting material and membrane in augmentation of dehiscence and fenestration defects encountered during dental implant surgery
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Background: Bone regeneration in dehiscence and fenestration defect can be improved with the use of platelet rich fibrin (PRF) that provides a scaffold for new bone regeneration. This study was conducted to assess the effectiveness of PRF as a graft material and membrane in dehiscence and fenestration defects. Materials and Methods: This prospective clinical study included patients who received dental implants that demonstrated peri-implant defects which were augmented using Leukocyte- PRF (L-PRF) or Advanced-PRF (A-PRF). Twenty four weeks postoperatively the defect resolution and the density of regenerated bone were assessed by CBCT and re-entry surgery. The assessment also included measurement of primary and secondary implant stability

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Publication Date
Wed Jun 02 2021
Journal Name
Indian Journal Of Forensic Medicine &amp; Toxicology
Estimation of the Cytotoxic Effects of Yucca Gloriosa Variegata Leaves Extract on Albino Mice
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Yucca gloriosa Variegata L. is a stemless. The whole plant of Y. gloriosa L. has vast medicinal uses. TheNative Americans and North New Mexico used a tea from the leaves and roots to treat asthma, headache,wound healing. As well as it was being consumed as daily dietary. All part of Y. gloriosa L. is rich in saponinsteroidal glycosides. Saponin extracts are well-known to be highly toxic. Hence, present study was carriedout to investigate the toxicity of saponin and estimate the LD50 value which helps in determining the safedose range for the drug that be used, as well as to determine hematological aspects and examine histologicaleffect. Different concentrations of saponin extract were injected into male mice (10,000, 8000, 6000, 400

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Publication Date
Mon Jun 01 2009
Journal Name
Engineering And Technology Journal
Synthesis and study of the Novel tetradented ligand type N2O2 and its complexes with (Mn (II) ,Co (II) ,Ni (II) and Cu(II)) ions
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A new Schiff base ligand Bis-1,4-di[N-3-(2-hydroxy-1-amino)- acetophenonylidene] benzylidene [L] and its complexes with (Mn(II) ,Co(II) ,Ni(II and Cu(II)) were synthesized . The ligand was prepared in two steps. In the first step a solution of (terphthalaldehyde) in methanol reacts under reflux with (p-aminoacetophenone) to give an intermediate compound [1-[3-({4-[(3-Acetyl-phenylimino)-methyl]-benzylidene}-amino)-phenyl]- ethanone which reacts in the second step with (2-Amino-phenol) giving the mentioned ligand. The complexes were synthesized by addition the corresponding metal salt solution to the solution of the ligand in methanol under reflux in (1:1) metal to ligand ratio. On the basis of, molar conductance, I.R., UV-Vis, HPLC, chlorid

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Publication Date
Fri Dec 31 2021
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
ADSORPTION POTENTIAL FOR A MIXTURE OF CHEMICALLY AND THERMALLY TREATED CLAYS TO REMOVE ORANGE G DYE FROM WASTE-WATER: ADSORPTION POTENTIAL FOR A MIXTURE OF CHEMICALLY AND THERMALLY TREATED CLAYS TO REMOVE ORANGE G DYE FROM WASTE-WATER
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This study examined the adsorption behavior of anionic dye (orange G) from aqueous solution onto the raw and activated a mixture of illite, kaolinite and chlorite clays from area of Zorbatiya (east of Iraq).The chemical treatment involved alkali and acid activation. The alkali activation obtained by treated the raw clay (RC) with 5M NaOH (ACSO) and the acid activation founded by treated it with 0.25M HCl (ACH) and 0.25M  (ACS). The thermal treatment carried out by calcination the produce activated clay at 750oC for acid activation and 105oC for alkali activation. Batch

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Publication Date
Wed Mar 31 2021
Journal Name
Indones. J. Chem.,
Synthesis and DFT Study of the Complexation of Schiff Base Derived Curcumin and L-Tyrosine with Al(III), Ag(I), and Pb(II) Metal Ions
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The multi-dentate Schiff base ligand (H2L), where H2L=2,2'-(((1,3,5,6)-1-(3-((l1-oxidaneyl)-l5-methyl)-4-hydroxyphenyl)-7-(4-hydroxy-3-methoxyphenyl)hepta-1,6-di ene-3,5-diylidene)bis(azaneylylidene))bis(3-(4-hydroxyphenyl)propanoic acid), has been prepared from curcumin and L- Tyrosine amino acid. The synthesized Schiff base ligand (H2L) and the second ligand 1,10-phenanthroline (phen) are used to prepare the new complexes [Al(L)(phen)]Cl, K[Ag(L)(phen)] and [Pb(L)(phen)]. The synthesized compounds are characterized by magnetic susceptibility measurements, micro elemental analysis (C.H.N), mass spectrometry, molar conductance, FT-infrared, UV-visible, atomic absorption (AA), 13C-NMR, and 1H-NMR spectral studies. The characterization of the

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Publication Date
Mon Nov 21 2022
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn: 2789-3219 )
Nanotechnology at the Molecular Level
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Materials with external dimensions of one or more nanometers are referred to as nanomaterials. These structures result from a number of manufacturing processes. They are used in many industries, including pharmaceuticals, which is the most significant one. Numerous variables, including size, shape, surface morphology, crystallinity, solubility, etc., affect physical properties. While new physical and chemical processes are being created constantly, the biological method is the ideal strategy for synthesizing nanoparticles since it is straightforward, safe, and economical. Different kinds of nanoparticles can be metabolically synthesized by a wide variety of biological sources, including plants, bacteria, fungi, and yeast. There are

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Publication Date
Thu Mar 30 2017
Journal Name
Journal Of Biotechnology Research Center
Study the Effects of Methotrexate with and without Vitamin A on Some Biochemical and Histological Parameters in Male Rabbits
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The present study aims to evaluate the effects of methotrexate (MTX) with and without vitamin A (Vit. A) on some biochemical parameters and histological structure in male rabbits liver. Twenty male rabbits weighing 1250-1480 gm were divided into four equal number groups. The first group was given 2 ml distilled water as control group. The second group was given MTX (20 mg/kg), the third group was given Vit. A (5000 IU), while the fourth group was given MTX (20 mg/kg) +Vit. A (5000 IU) in alternative days. Following four weeks of treatment, lipid profile total cholesterol (TC), triglycerides (TG), high-density lipoprotein (HDL), [low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL)]; in addition to thyroid hormones tr

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