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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
Mon Jun 05 2023
Journal Name
Journal Of Engineering
Potential Use of Recycled Asphalt Pavement (RAP) in Hot MixAsphalt
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The objective of the present paper is to examine the effect of Recycled Asphalt Pavement (RAP) on marshall properties and indirect tensile strength of HMA through experimental investigation. A mixture with 0% RAP was used as a control mix to evaluate the properties of mixes with 5%, 10%, and 15% RAP. One type of RAP was brought from Bab Al-moadam’s road in Baghdad for this purpose. The experimental testing program included Marshall and Indirect Tensile Strength tests. The results indicated that the bulk density, flow and VFA increase with the increasing of the percentage of RAP, while increasing in RAP results decreases in VTM and VMA values. Furthermore, the stability is changed from 10.1 kN for the control mix to12, 13.6 and 11.7 kN

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Publication Date
Tue Nov 01 2022
Journal Name
Japanese Dental Science Review
Pathogenesis of periodontitis – A potential role for epithelial-mesenchymal transition
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Publication Date
Tue Nov 01 2022
Journal Name
Japanese Dental Science Review
Pathogenesis of periodontitis – A potential role for epithelial-mesenchymal transition
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Epithelial mesenchymal transition (EMT) is a process comprising cellular and molecular events which result in cells shifting from an epithelial to a mesenchymal phenotype. Periodontitis is a destructive chronic disease of the periodontium initiated in response to a dysbiotic microbiome, and dominated by Gram-negative bacteria in the subgingival niches accompanied by an aberrant immune response in susceptible subjects. Both EMT and periodontitis share common risk factors and drivers, including Gram-negative bacteria, excess inflammatory cytokine production, smoking, oxidative stress and diabetes mellitus. In addition, periodontitis is characterized by down-regulation of key epithelial markers such as E-cadherin together with up-regulation of

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Publication Date
Mon Nov 02 2020
Journal Name
International Journal Of Pharmaceutical Research
Evaluation of Serum Adropin Levels in Nonalcoholic Fatty Liver Disease as A Complication of Hypothyroidism In Iraqi Patients
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Publication Date
Fri Feb 20 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Immunohistochemical expression of MMP1 and TIMP1 as markers of migration in Hodgkin’s and non-Hodgkin’s lymphoma of the head and neck region (A comparative study)
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Background: Malignant lymphoma is a term that describes primary tumors of the lymphoreticular system, almost all of which arise from lymphocytes.MMP-1 is the most ubiquitously expressed interstitial collagenase, a subfamily of MMPs that cleaves stromal collagens. It is also called collagenase-1.TIMPs which inhibits MMP activity and thereby restrict extracellular matrix breakdown, TIMP-1 is a stromal factor that has a wide spectrum of functions in different tissues. Material and Methods: This study was performed on (68) formalin-fixed, paraffin-embedded blocks, histopathologically diagnosed as lymphoma (head and neck lesions). Immunohistochemical staining of MMP1and TIMP1 was performed on each case of the study sample. Results: The expressio

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Publication Date
Fri Feb 20 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of some salivary enzymes levels in type 2 diabetic patients with chronic periodontitis (Clinical and biochemical study)
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Background: Diabetic patients have been reported to be more susceptible to gingivitis and periodontitis than healthy subjects. Many intracellular enzymes like (alkaline phosphatase- (ALP), aspartate aminotransferase- (AST) and alanine aminotransferase- (ALT) that are released outside cells into the gingival crevicular fluid (GCF) and saliva after destruction of periodontal tissue during periodontitis. This study was conducted to determine the periodontal health status and the levels of salivary enzymes (ALP, AST and ALT) of the study and control groups and to correlate the levels of these enzymes with clinical periodontal parameters in each study group. Subjects, Materials and Methods: One hundred subjects were enrolled in the study, with a

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Publication Date
Fri Feb 20 2026
Journal Name
Journal Of Physical Education
Consecutive Case Study of Detraining On Some Functional, Physical, Body and Compound Skills Variables In Advance Basketball Players
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Publication Date
Sun Sep 04 2016
Journal Name
Baghdad Science Journal
A Study the Effect of TiO2 Nanoparticles Combination with Antibiotics and Plant extracts Against Some Gram Negative Bacteria
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Titanium dioxide TiO2 has been widely utilized in cleaning and sterilizing material for many clinical tools sanitary ware, food tableware and cooking and items for use in hospitals. Titanium dioxide TiO2 non toxicity and long term physical and chemical stability. It has been widely used decomposition of organic compounds and microbial organisms such as cancer cell, viruses and bacteria as well as its potential application in sterilization of medical devices. The aim of the study the effect of titanium dioxide TiO2 on some Gram negative bacteria and study their effects on some virulence factors and chromosomal DNA.In this study, we obtained (E. coli ? Proteus mirabilis, Proteus vulgaris ? Pseudomonas aeruginosa ? Klebsiella pneumonia and Ac

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Publication Date
Tue Nov 17 2020
Journal Name
Annals Of Tropical Medicine And Public Health
Correlation Study of Aromatase, Some Sex Hormones, and Body Mass Index Among Iraqi Patients with Polycystic Ovary Syndrome
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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Effect Study the of Acute toxoplasmosis on Some Blood and Serum Parameters in Pregnant Women in Baghdad City
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In this study the rate of infection in acute and chronic Toxoplasma gondii parasite that causes toxoplasmosis was determined. This study was Included 120 blood samples that collected from pregnant women revisions to some clinics and laboratories in Baghdad civil as well as 10 blood samples from non-infected women as a control group. All blood samples were collected in the first three months of the pregnancy period for detection toxoplasmosis by using serological tests of test kit ( Toxo , IgG.,Toxo , IgM ). To detect antibodies specialized type of IgG &IgM in acute and the chronic infection by Electro Clia manner using a Roche Cobas e411. The results showed that the total infection rate was (55.83)%, the rate of infection in acu

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