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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
Thu Jan 01 2015
Journal Name
Iraqi National Journal Of Chemistry
Synthesis of some benzofuran-based pyrazoline, isoxazoline, pyrmidine, cyclihexenone and indazole derivatives
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In the present study benzofuran based chalcones 1 (a, b) are synthesized by condensing aromatic aldehydes with 2-acetylbenzofuran in the presence suitable base. These chalcones are very useful precursors for the synthesis of pyrazoline, isoxazoline, pyrmidine, cyclohexenone and indazole derivatives. All these compounds are characterized by their melting points, FTIR and 1 HMNR (for some of them) spectral dat

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Publication Date
Wed Mar 24 2021
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Evaluating the anti- Pseudomonas Aeroginosa Efficacy and Potential Cytotoxicity of Nerium Oleander Alcoholic Extract
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Nerium oleander known as oleander has belonged to the poisonous plants its habitat in a tropical andsubtropical region. The chemical analysis with GC-Mass of the alcoholic extract of oleander leaves revealedthat this plant has many chemical compounds more than 80 compounds and high-peaks about 29 compoundswhich are represented by alkaloids, phenol, terpenes, and fatty acid. HPLC analysis showed many essentialoils that have many biological effects.To evaluate the antibacterial activity of the alcoholic extract of N. oleander against locally isolatedPseudomonas aeroginosa the broth micro-dilution method was adapted to different concentrations werestarted from 3.9 to1000 mg/ml. The results revealed that the alcoholic extract has antiba

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Publication Date
Mon Jan 01 2024
Journal Name
Tropical Journal Of Natural Product Research
Cytotoxic Potential of Neem (Azadirachta indica A. Juss) Oil
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An increasing interest is emerging in identifying natural products to overcome drug resistance in cancer patients. In this context, the present study was conducted to investigate the cytotoxic effects of neem plant (Azadirachta indica) oil in three different biological models (breast cancer cell lines, Allium cepa root tip, and mice vital organs). The cytotoxic potential of the neem oil was evaluated with two human cell lines (MCF7 and MDA-MB231) and an Allum cepa root tip bioassay. Histopathological analysis was conducted on the neem oil-treated and untreated control mice. The results revealed an anti-proliferative effect for neem oil on both estrogen receptor-positive (MCF7) and estrogen receptor-negative (MDA-MB231) breast cancer cell li

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Publication Date
Sun Dec 31 2023
Journal Name
Tropical Journal Of Natural Product Research
Cytotoxic Potential of Neem (Azadirachta indica A. Juss) Oil
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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of new derivatives of Ceftazidime as possible Prodrugs
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Five new ceftazidime derivatives were designed and synthesized in an attempt to improve the acid stability and may increase the spectrum of ceftazidime. The synthesized compounds included;  Schiff base of ceftazidime (compound 1), ceftazidime lysine amide Schiff base (compound 2), ceftazidime lysine amide (compound 3), ceftazidime-di-lysine amide Schiff base (compound 4) and ceftazidime-di-lysine amide (compound 5). New ceftazidime derivatives were successfully prepared characterized and identified using spectral and elemental microanalysis (CHNS) analyses and the results comply with the calculated measurements.

Compounds 1 and 2 were subjected to a stability study in phosphate buffer (0.2M, pH 7.4) and in KCl/HCl buffer (0.

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Publication Date
Wed Jan 01 2025
Journal Name
Aip Conference Proceedings
Synthesis and evaluation of chalcone derivatives for antimicrobial and antioxidant activities using microwave-assisted methodology
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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
Mon Mar 01 2010
Journal Name
Journal Of Kerbala University
Synthesis And Biological Activity Of Some New Compounds Containing 1,2,4-Triazole And Their Derivatives
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Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-

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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Pyridine and Pyrimidine Derivatives and Studying Their Biological Activities
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Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy

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Publication Date
Sun Mar 17 2019
Journal Name
Baghdad Science Journal
The Potential of some Plant Extracts as Radical Scavengers and Dipeptidyl Peptidase-4 Inhibitors
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Seeds, beans, leaves, fruit peel and seeds of five plants (Ferula assa-foetida, Coffea robusta, Olea europaea, Punica granatum and Vitis vinifera, respectively) were extracted with four solvents (distilled water, 80% methanol, 80% acetone and a mixed solvent that included methanol, ethanol, acetone and n-butanol at proportions 7:1:1:1). Such manipulation yielded 20 extracts, which were phytochemically analyzed for total polyphenols (TP) and flavonoids (TF). The DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity (RSA) and DPP-4 (dipeptidyl peptidase-4) relative inhibition activity (RIA) were also assessed for each extract. The results revealed that mixed solvent extract of V.

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