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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 Aug 24 2026
Journal Name
Recent Advances In Drug Delivery And Formulation
Development of Lyophilized Ebastine-Loaded Novasome Tablets: Comprehensive Physicochemical Characterization and In Vitro/In Vivo Release Evaluation
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Introduction/Objective:

Ebastine, a second-generation H1 antihistamine, exhibits poor aqueous solubility and consequently low oral bioavailability, limiting its clinical therapeutic efficacy. Novasome is an advanced vesicular nanocarrier system that offers a promising approach to enhance the solubility and dissolution behavior of a poorly water solubility drug. Therefore, this study aimed to develop, optimize, and characterize ebastine-loaded novasomes and to compress them into tablets to enhance drug solubility, dissolution, and oral bioavailability.

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Publication Date
Wed Mar 18 2020
Journal Name
Baghdad Science Journal
Synthesis of Six and Seven-membered Heterocyclic Molecules Containing an Adamantyl Fragment and an X-ray Crystal Structure of (E)-N-(adamantan-1-yl)-1-(3-nitrophenyl)methanimine
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       Our work included a synthesis of three new imine derivatives—1,3-thiazinan-4-one, 1,3-oxazinan-6-one and 1,3-oxazepin-4,7-dione—which contained an adamantyl fragment. These were produced via the condensation of the Schiff`s base (E)-N-(adamantan-1-yl)-1-(3-aryl)methanimine with 3-mercaptopropanoic acid; 3-chloropropanoic acid; and maleic, citraconic anhydride, respectively. These new imines were prepared via the condensation of adamantan-1-ylamine and 3-nitro-, 3-bromobenzaldehyde in n-BuOH. We obtained a good yield of products. FTIR, 1H NMR spectroscopy and C.H.N.S analysis were used to diagnostic the products. The molecular structure of (E)-N-(adamantan-1-yl

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Publication Date
Mon Dec 31 2018
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
EFFECT OF ADDING TWO (Curcuma longa) LEVELS OF CURCUMA ON SOME PRODUCTIVE AND PHYSIOLOGICAL CHARACTERISTICS FOR QUAIL JAPANESE.: EFFECT OF ADDING TWO (Curcuma longa) LEVELS OF CURCUMA ON SOME PRODUCTIVE AND PHYSIOLOGICAL CHARACTERISTICS FOR QUAIL JAPANESE.
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A study carried out in quail’s field owned by the Department of Animal production/ Collage of Agriculture / Tikrit University. For the period 14/ 5/ 2016 to 4/ 6/ 2016 in order to study the effect of adding Curcuma longa - to the diet of quails - on some productive and physiological characteristics of the Japanese quail birds bred for meat production. Using (48) quail birds which are two weeks old provided by Department of Agricultural Research. The birds were divided randomly after weighing them into three treatments; four replicate treatments for (4 bird/ replicate). The treatments as follows: (T1) control group (fed diet without any supplement), second (T2) and third (T3) groups were fed diet supplemental 4.5 and 9g Curcuma powder /

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
The concept of suspense and mystery with some references to dickens s Novels ; A tale of two cities and Great expectations
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Publication Date
Mon Aug 26 2024
Journal Name
Iraqi Journal Of Agricultural Sciences
EFFECT OF USING AVOCADO, CHIA OIL AND THEIR MIXTURE IN BROILER DIETS ON PRODUCTIVE PERFORMANCE AND SOME CHEMICAL CHARACTERISTICS OF MEAT
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This study was conducted in the field of the Poultry Research Station of the animal resources Department / office of Agricultural Research / Ministry of Agriculture from the period 4th April to16th May2021.This study was aimed to investigate the effect of using avocado and chia oil and their mixture in broiler diets on the final productive performance and meat cholesterol concentration and measuring meat oxidation indicators after storing it for 60 days. 300 one-day-old (Ross308) chicks were fed on diets that used avocado oil and chia with percentages of 0, 0.2, 0.4, 0.6%, respectively, and their mixture consisting of 0.0, 0.1, 0.2, 0.3 each of avocado and chia oil (50% avocado + 50% chia oil). The experiment included 10 treatments

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Publication Date
Mon Feb 10 2020
Journal Name
Iraqi Journal Of Soil Sciences
Spatial Variability of Some Soil Chemical and Fertility Properties in Hydrosequences through Grain Crops Growing Areas of Najaf and Alqadissiya Provinces
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Kiffil Shinafiya project was selected as it’s been conducted and covering the areas of grain crops agriculture in Najaf and Qadissiya provinces. Lands of this project are considered as a part of the Mesopotamian plain located in between N32⁰ 15′, N31⁰ 30′ and E44⁰ 44’, E44⁰ 20′. Three hydrosequences were disclosed with three transects (T1, T2, T3) in the area of study. The first hydrosequence was perpendicular on the other two sequences. Fifteen pedons were outcropped, five pedons in each transect in addition to eighteen more surface samples to be a total samples of 33 locations. Pedons were morphologically described due to soil survey manual (Soil Survey Staff, 2017). Spatial distribution of soil salinity showed that the

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Publication Date
Tue May 16 2023
Journal Name
Journal Of Engineering
Critical Evaluation of City Streets
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 The diverse urban spaces of the streets is an important part of the city's physicist configuration and a link between architectural and civilizational communication through time starting from the historic towns down to the contemporary cities, within the proposals of the future cities. From general observations and literature review a research problem is crystallized as some directions not arbitrary rational when expansion and the growth of cities, and other measures wrong or the existence of some incorrect actions and processes related to the cities planning as a categorizing the goals and priorities in city plan.The streets were constitute a high proportion of the total area of cities, where up to over 30% in major cities. These

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Publication Date
Wed Jan 31 2024
Journal Name
Iraqi Geological Journal
Identification of Lateritic Nickel Deposits Potential in the Kokoe Area, Kabaena Island, Central Buton Regency, Southeast Sulawesi Province, Indonesia
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The study is situated in the Kokoe Region of Central Buton Regency, Southeast Sulawesi, specifically in the southern part of Kabaena Island. Its primary objective is to assess the potential of nickel laterite in the designated area. The research methodology involved microscopic analysis of bedrock using a polarizing microscope, examining the drilling data, including logging descriptions, and utilizing XRF geochemical analysis (Ni, Fe, Al2O3, Co, Mg, and SiO2) from 32 drilling sites. Both elementary grade and laterite profiles were visualized using Strater 5 software to simplify the representation of laterite profiles. Petrographic analysis divided the bedrock into two lithological units: serpentinized lherzolite and serpentinite. Th

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Publication Date
Tue Jul 21 2015
Journal Name
Diyala Journal For Pure Sciences
Synthesis and biological studies 0fCo(||)،Ni(||)،Cu(||) And Zn(||)complexes with New compound N-(2,3-dioxoindolin-1-yl)_N_methyl benzamide
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Synthesis and biological studies 0fCo(||)،Ni(||)،Cu(||) And Zn(||)complexes with New compound N-(2,3-dioxoindolin-1-yl)_N_methyl benzamide

Publication Date
Sat Jul 08 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Effect of Coumarin Derivatives(compounds) on the Vibrio cholerae Isolates from Different Clinical Iraqi Sources
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From a large number of bacterial samples collected from different hospital in Iraq in central  health laboratory ,only ten isolates were identified primary as Vibrio. A number of  morphology and biochemical test were carried out to complete this identification that showed all bacterial isolates were related to Vibrio cholerae .In this study  all Vibrio isolates were investigated for Bio typing and the result showed that all (10) isolate were related to (Eltor biotypes) .Also, the susceptibility test towards eight antibiotics were carried  out .

Results shows that  ciprofloxacin , Norfloxacin, Erythromycin, Ampicillin,  ceftriaxone  and Amikacin were the most effective

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