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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 Jul 01 2024
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Evaluation of some Biochemical and Hematological Parameters in Patients with Chronic Kidney Disease
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Background: Chronic kidney disease is a condition that results from an indefinite change in the structure and function of the kidneys. A slow, steady progression characterizes it and is irreversible.  Objectives: This study aims to evaluate the findings of certain biochemical and hematological tests in samples from Iraqi CKD patients.  Methods: This study included 90 subjects, where 70 patients with chronic kidney disease and 20 healthy individuals. Blood samples were collected from the patients during their visits to Ghazi Al-Hariri Surgical Specialties' Hospital- Medical City, Baghdad, Iraq. Age, sex and body mass index were assessed for each participant followed by renal function tests [serum blood urea, creatinine, uric acid a

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Publication Date
Fri Nov 25 2022
Journal Name
Baghdad Science Journal
Evaluation of Some Antioxidants and Oxidative Stress Tests in Iraqi Lung Cancer Patients
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Vitamin K-dependent protein (VKDP) contributes to the development of lung cancer. The purpose of this research was to better understanding of the role of blood matrix Gla protein (MGP), VKDPs, Malondialdehyde (MDA), Superoxide dismutase (SOD) and Vitamin K (Vit K) in Iraqi patients with lung cancer before and after the first cycle of chemotherapy. Blood samples were collected from Al amal National Hospital for cancer treatment from October 2021 to May 2022, and a total of 80 samples were collected, divided into two groups (40 patient before taking a chemotherapy and 40 patients after taking chemotherapy), ranging in age from 20 to 45 years old. The results showed that although there were highly statistically significant differences in MD

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Publication Date
Fri Aug 18 2023
Journal Name
Medicinal Chemistry Research
New tolfenamic acid derivatives with hydrazine-1-carbothioamide and 1,3,4-oxadiazole moieties targeting VEGFR: synthesis, in silico studies, and in vitro anticancer assessment
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Publication Date
Tue Mar 15 2022
Journal Name
Journal Of Baghdad College Of Dentistry
In vitro cytotoxic effect of annona squamosa pulp ex-tract as a mouthwash for children on human normal cell line
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Background: Fruits and their by-products are the primary sources of bioactive chemicals in plants. Because of its phytochemical richness, Annona squamosa fruits have gained the alertness of people willing in health-promoting diets. The purpose of this in vitro study was to evaluate the cytocompatibility effect of ethanolic crude extract of Annona squamosa pulp against a human normal cell line as a mouthwash for children. Material and method: The ethanolic extract of Annona squamosa pulp was extracted using the ultrasonic method and then lyophilized to make it powder. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) test was performed to investigate the cytotoxic activity of the pulp extract on a human normal cell l

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Publication Date
Mon Jan 01 2024
Journal Name
Biomed Research International
Potential Association of Maker Expression of Low‐Density Neutrophils and Their Phenotypes in Patients with Periodontitis: Control Study
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Background. Neutrophils play an important role in maintaining periodontal status in conditions of healthy homeostasis. They achieve their surveillance function by continuously migrating to the gingival sulcus and eradicating periodontal pathogens. In addition, neutrophils are considered an integral element in the pathogenesis of periodontal diseases. Among several neutrophil subsets, low‐density neutrophils (LDN) have recently received attention and are linked with cancer, immunological, inflammatory, and infectious diseases. However, the presence, phenotypes, and potential role of LDN in the pathogenesis of periodontitis have not yet been investigated. Objectives. To investiga

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Publication Date
Mon Jan 01 2024
Journal Name
Kafkas Universitesi Veteriner Fakultesi Dergisi
Assessment of In-vitro Cytotoxicity and In-ovo Virucidal Antiviral Efficacy of Various Plant Extracts and Bioactive Molecules
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Publication Date
Thu Jun 15 2023
Journal Name
Romanian Neurosurgery
Sellar hematoma as a new potential radiological clue for superior hypophyseal artery aneurysm rupture
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Background. In cases of spontaneous subarachnoid haemorrhage (SAH) with multiple intracranial aneurysms (MIAs) detected on angiography, some radiological clues assist in determining the site of a ruptured aneurysm which is bleeding is quite beneficial for the selection of the best treatment strategy. Case description. We report a case of a 60 years old patient who presented with spontaneous SAH, sellar hematoma, and three different aneurysms detected in angiography. Although the right Posterior communicating artery (PcomA) aneurysms showed Murphy’s teat on angiography intraoperatively, we discovered that the right superior hypophyseal aneurysm (SHA) was the source of the index bleeding. Both aneurysms were clipped successfully. Co

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Publication Date
Sat Dec 01 2012
Journal Name
Journal Of Al-nahrain University Science
Synthesis and Characterization of Some Metals Complexes of {N-[(Benzoyl Amino)-Thioxo Methyl] Proline}
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Publication Date
Tue Nov 14 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
[PDF] من iasj.net Synthesis and Characterization of Some New Transition Metal Complexes of Amino
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الوصف New complexes of Cu (ll), Ni (II)„Co (II), and Zn (ll) with 2-amino-5-p-Flouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(FT-IR)„UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Mon Aug 01 2022
Journal Name
Baghdad Science Journal
The Potential Role of Soil Bacteria as an Indicator of Heavy Metal Pollution in Southern, Iraq
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       The present study was performed to spotlight the potential role of soil bacteria in the Al-Rumaila oil field as a bioindicator of heavy metals pollution. For this purpose, nine soil samples were collected from different sites, with 20cm depth, to assess the pollution status depending on the total and available concentrations of heavy metals.  The result indicates pollution of the studied soils with the following metals: Cd, Cu, Fe, Zn, and Pb. The mean of total concentration for all studied metals was higher than the allowed maximum limit based on the international limit:(3.394, 3.994, 39.993, 8844.979,150.372, and 103.347 µg/g), respectively. While measuring the total Metal concentration is important in determining the de

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