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Synthesis of 5‐Fluorouracil–Naproxen Conjugates as a Mutual Prodrug for Targeting Cancer Tissues
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Abstract<p>A new 5‐fluorouracil–naproxen conjugate is synthesized as a mutual prodrug for targeting cancer tissues. The structure of the target compound and their intermediate are characterized by their melting point, IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, and elemental microanalysis. The cytotoxic activity is preliminarily evaluated using nonsmall lung cancer CRL‐2049, human breast cancer CAL‐51, and one type of normal cell line; rat embryo fibroblast cell line. The synthesized compound shows a good cytotoxic effect at the cancer cell and no significant effect at rat embryo fibroblast cell line.</p>
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Publication Date
Sun Mar 03 2013
Journal Name
Journal Of Al-nahrain University
Synthesis and Characterization of Some New 1,2,3-Triazole, Pyrazolin-5-one and thiazolidinone Derivatives
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Five membered heterocyclics derivatives were synthesized in this work by three routes. The first route includes the synthesis of N-benzoic acid 1,2,3,-triazole derivatives (3),(4) by diazotation of methyl-2-amino benzoate and treating the resulted salt (1) with sodium azide and ethyl acetoacetate or acetyl acetone, respectively. In the second route, derivatives of pyrazole (8) pyrazolin-5-one (9), (10) were prepared by the reaction of the salt (1) with some active methylene compounds to give the corresponding hydrazones derivatives (5-7) which then they were treated with hydrazine hydrate. The third route afforded the synthesis of three derivatives (12), (15a), (15b) of thiazolidinone by two different methods. AII compounds were confirmed b

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Publication Date
Sun May 28 2017
Journal Name
Ibn Al-haitham Jour. For Pure & Appl. Sci
Synthesis of Some New Heterocyclic Fused Rings Compounds Based on 5-Aryl-1,3,4-Oxadiazole
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The work includes synthesis and characterization of some new heterocyclic compounds, as flow: The compound (3) (5-(4-chlorophenyl) -2-hydrazinyl-1,3,4-oxadiazole was synthesized by using two methods; the first method includes the direct reaction between hydrazine hydrate 80% and 5-(4-chlorophenyl)-2- (ethylthio) 1,3,4-oxadiazole (1), the second method involves converting 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-amine (2) to diazonium salt then reducing this salt to compound (3) by stannous chloride. Compound (3) was used as starting material for synthesizing several fused heterocyclic compounds. The compound 6-(4- chlorophenyl)[1,2.4] triazolo [3,4,b][1,3,4] oxadiazole-3-(2H) thione (compound 4) was synthesized from the reaction of compo

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Publication Date
Fri Mar 25 2016
Journal Name
Oriental Journal Of Chemistry
Synthesis and Antioxidant Ability of New 5-amino-1,2,4-Triazole Derivatives Containing 2,6-dimethoxyphenol
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4-amino-3-(4-(((4-hydroxy-3,5dimethoxybenzyl)oxy)methyl)phenyl)-1,2,4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoyl)hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1,2,4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to scree

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Publication Date
Wed Sep 01 2021
Journal Name
Acta Pharmaceutica Sinica B
Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5
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Publication Date
Fri Apr 27 2012
Journal Name
Al-qadisiyah Journal For Science
Synthesis and Characterization of azo Compound 5-(2-Benzoic acid azo)-8-hydroxy quinoline as Bidentate Ligand and It’s Complexeswith Co (II), Ni (II) and Cu (II) .
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Coupling reaction of 2-amino benzoic acid with the 8-hydroxy quinoline gave the azo ligand (H2L): 5-(2-benzoic acid azo )-8-hydroxy quinoline.Treatment of this ligand with some metal ions (CoII, NiII and CuII ) in ethanolic medium with a (1:2) (M:L) ratio yielded a series of neutral complexes with general Formula[M(HL)2],where: M=Co(II), Ni(II) and Cu(II), HL=anion azo ligand (-1).The prepared complexes were characterized using flame atomic absorption,FT-IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements.

Publication Date
Sun Jun 20 2010
Journal Name
Al-qadisiya Journal For Science
Synthesis 4-phenyl -1-alkyl-1,2,4-triazoline-5-one derived from D- fructose
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The aim of the present work is the synthesis of new carbohydrate derivatives containing 1,2,4-triazole from D-fructose . To obtain these derivatives, the diacetone fructose (1 ) was chosen as the starting material, which was obtained from the reaction of anhydrous fructose with dry acetone in presence of anhydrous ferric chloride. Oxidation of ( 1) with potassium permanganate in potassium hydroxide solution gave the acid ( 2). Esterification of the acid with dimethyl sulphate gave the methyl ester (3 ). Treatment of the methyl ester (3 ) with hydrazine hydrate gave the hydrazide (4 ), which is the desired Chiron. The hydrazide (4 ) was used for the preparation of 1,2,4-triazole-5-one (6 ) derivative. These compounds was synthesized by the i

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Publication Date
Wed Mar 30 2022
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Catalytic Conversion of Glucose into 5-hydroxymethyl furfural over Spent Dry Batteries as Catalysts
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Biomass is a popular renewable carbon source because it has a lot of potential as a substitute for scarce fossil fuels and has been used to make essential compounds like 5-hydroxymethylfurfural (HMF). One of the main components of biomass, glucose, has been extensively studied as a precursor for the production of HMF. Several efforts have been made to find efficient and repeatable procedures for the synthesis of HMF, a chemical platform used in the manufacturing of fuels and other high-value compounds. Sulfonated graphite (SG) was produced from spent dry batteries and utilized as a catalyst to convert glucose to 5-hydroxymethylfurfural (HMF). Temperature, reaction time, and catalyst loading were the variables studied. When dimethyl sulfo

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Publication Date
Wed Jun 26 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Acetylenic Derivatives of a Substituted 1, 3, 4-Thiadiazole as Antibacterial Agents
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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Micro encapsulation of Naproxen By Complex Coacervation and Aqueous Colloid Dispersion Part ( 1 )
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Naproxen is a non steroidal anti inflammatory and antipyretic drug which has local irritation effect  on  the  stomach, and  unpleasant taste,  besides bad   flowability and light sensitivity .The drug was prepared as microcapsules by complex coacervation method using acacia-gelatin coating materials , and aqueous colloid polymer dispersion method ( ACPD ), using ethyl cellulose and sodium alginate coating materials . The results indicated that microcapsules prepared by 2:1  core:wall ratio is the best for both methods, with an average encapsulation efficiency (75%) and avarege yield (90%) .

Moreover the drug release was affected mainly by core : ratio ,pH enviroment and method of microenca

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
Deep Learning Techniques in the Cancer-Related Medical Domain: A Transfer Deep Learning Ensemble Model for Lung Cancer Prediction
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Problem: Cancer is regarded as one of the world's deadliest diseases. Machine learning and its new branch (deep learning) algorithms can facilitate the way of dealing with cancer, especially in the field of cancer prevention and detection. Traditional ways of analyzing cancer data have their limits, and cancer data is growing quickly. This makes it possible for deep learning to move forward with its powerful abilities to analyze and process cancer data. Aims: In the current study, a deep-learning medical support system for the prediction of lung cancer is presented. Methods: The study uses three different deep learning models (EfficientNetB3, ResNet50 and ResNet101) with the transfer learning concept. The three models are trained using a

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