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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
Sat Jun 01 2024
Journal Name
Journal Of Research In Dental And Maxillofacial Sciences
Relationship between Third Molar Impaction and Extraction, and Awareness about the Associated Potential Risks
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Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis and Identification of New 2-Substituted-1,3,4-Oxadiazole Compounds from Creatinine and Study Their Antioxidant Activities
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Publication Date
Sun Oct 15 2023
Journal Name
Sumer 4
CYTOTOXIC IMPACT OF OUTER MEMBRANE NANOVESICLES (OMVS) ON OVARIAN CANCER
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This study focused on extracting the outer membrane nanovesicles (OMVs) from Escherichia coli BE2 (EC- OMVs) by ultracentrifugation, and the yield was 2.3mg/ml. This was followed by purification with gel filtration chromatography using Sephadex G-150, which was 2mg/ml. The morphology and size of purified EC-OMVs were confirmed by transmission electron microscopy (TEM) at 40-200 nm. The nature of functional groups in the vesicle vesicle was determined by Fourier transforms infrared spectroscopy (FT-IR) analysis. The antitumor activity of EC-OMVs was conducted in vitro by MTT assay in human ovarian (OV33) cancer cell line at 24,48 and 96hrs. The cytotoxicity test showed high susceptibility to the vesicles in ovarian compared to normal

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Publication Date
Fri Dec 23 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Aspirin Derivatives Exploration: A Review on Comparison Study with Parent Drug
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In recent decades, drug modification is no longer unusual in the pharmaceutical world as living things are evolving in response to environmental changes. A non-steroidal anti-inflammatory drug (NSAID) such as aspirin is a common over-the-counter drug that can be purchased without medical prescription. Aspirin can inhibit the synthesis of prostaglandin by blocking the cyclooxygenase (COX) which contributes to its properties such as anti-inflammatory, antipyretic, antiplatelet and etc. It is also being considered as a chemopreventive agent due to its antithrombotic actions through the COX’s inhibition. However, the prolonged use of aspirin can cause heartburn, ulceration, and gastro-toxicity in children and adults. This review article hi

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Publication Date
Tue Jan 01 2019
Journal Name
Biochemical And Cellular Archives
Phenotypic and molecular detection of Escherichia coli efflux pumps from UTI patients
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Publication Date
Wed Apr 01 2020
Journal Name
Indian Journal Of Ecology
Isolation and molecular identification of yersinia entercolitica in Bovine Meat in Iraq
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Publication Date
Tue Apr 01 2025
Journal Name
Iop Conference Series: Earth And Environmental Science
Molecular Detection and Antiserum Preparation of Begomoviruses Infecting Zucchini Squash in Iraq
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Abstract<p>Begomoviruses infecting zucchini squash were investigated. Leaf samples were collected from zucchini squash growing areas in Baghdad (Jhadryaa and Yusufiyah), Babylon (Jibela and Mahmudiyah) and Diyala (Khan Bani Saad) Provinces. Samples were screened for the presence of begomoviruses using polymerase chain reaction (PCR) and Deng genus specific primers. Sixteen out of 40 samples were begomovirus positive. Sequence analysis confirmed the detection of Tomato leaf curl Palampur virus (TLCPALV) <italic>Begomovirus solanumpalampurense</italic>, Squash leaf curl virus (SLCuV) <italic>B. cucurbitapeponis</italic> and Tomato yellow leaf curl virus (TYLCV) <italic>B. </italic></p> ... Show More
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Publication Date
Mon Dec 28 2020
Journal Name
The Iraqi Journal Of Veterinary Medicine
Serological and Molecular Phylogenetic Detection of Coxiella burnetii in Lactating Cows, Iraq
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This study is carried out to investigate the prevalence of Coxiella burnetii (C. burnetii) infections in cattle using an enzyme-linked immunosorbent assay (ELISA) and polymerase chain reaction (PCR) assay targeting IS1111A transposase gene. A total of 130 lactating cows were randomly selected from different areas in Wasit province, Iraq and subjected to blood and milk sampling during the period extended between November 2018 and May 2019. ELISA and PCR tests revealed that 16.15% and 10% of the animals studied were respectively positive. Significant correlations (P<0.05) were detected between the positive results and clinical data. Two positive PCR products were analyzed phylogenetically, named as C. burnetii IQ-No.5 and C. burnet

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Publication Date
Fri Jan 01 2021
Journal Name
Bulgarian Journal Of Veterinary Medicine
First isolation and molecular phylogenetic analysis of Coxiella burnetii in lactating cows
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Q fever is an infectious disease of animals and humans, caused by globally distributed C. burnetii. In Iraq, there are no previous studies associated with the detection of the organism in cattle. An overall of 130 lactating cows were submitted to direct collection of milk samples. Initially, the samples of milk were tested using the molecular polymerase chain reaction (PCR) assay targeting three genes (16S rRNA, IS1111a transposase, and htpB). However, positive results (18.46%; 24/130) were detected only with the 16s rRNA gene. Concerning risk factors, the highest prevalence of C. burnetii was showed in the district of Badra (42.86%), whereas the lowest - in Al-Numaniyah and Al-Suwaira districts (P=0.025). There was no significant v

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Publication Date
Sun Jan 01 2017
Journal Name
International Journal Of Economic Research
Credit derivatives: Do they matter to avoid credit exposure? (Some evidences from the US market)
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Credit derivatives (CDs) have been increasingly acknowledged as an important requirement to hedge and transfer credit risk CR. Nonetheless, they have been extensively criticized for destabilizing the whole economic system bringing about the latest subprime credit crisis. The study’s main aim is to investigate the reason for the use of (CDs), whether it is used for hedging or trade purpose, for four of the US international financial institutions that had made it through the 2007 crisis to resume functioning post-crisis. This will be for three different and critical periods, namely the pre, during and after crisis periods (Q1, 2000-Q1, 2014). Adopting the SUR technique, the investigation of the factors that influence the net position of (CD

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