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bijps-1639
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 Dec 02 2017
Journal Name
International Food Research Journal
Extraction and purification of cytotoxic compounds from Premna serratifolia L.(bebuas) for human breast cancer treatment.
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Publication Date
Tue Jan 01 2013
Journal Name
European Journal Of Experimental Biology
Cytotoxic and apoptotic activity of leinamycin Produced by Streptomyces atroolivaceous THS-44 isolate from Iraqi soli
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Leinamycin is a thiol dependent DNA alkylating agent which shows very potent activity against various cancer cell lines. This natural compound forms guanine adducts (N7) in DNA which are converted into a basic sites and simultaneously generates Reactive Oxygen Species (ROS), to produce DNA strand breaks in human cancer cells. In present study, eight different strains isolated from Iraqi soils were taxonomically assigned as Streptomyces.atroolivaceous. Remarkably the strain named as THS-44 was distinguished in productivity in comparison with other strains; the amount of leinamycin was 50.98 mg/l. In this study, we assessed the cytotoxic activity of leinamycin against RD and ANM3 cancer cell line in compare with REF cell line as a normal cont

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Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Quantitative Determination and Cytotoxic Effect of Oleanolic Acid from Olea europaea Leaves Extract Cultivated in Iraq
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Since its first description as a cytotoxic agent, Olea europaea leaves extract gained significant popularity against human breast cancer, ethyl acetate extract of Olea europaea leaves obtained by acid hydrolysis method was evaluated in vitro as cytotoxic agent against new human breast cancer (AMJ13) cell line, using the MTT assay. One main pentacyclic triterpenoid; oleanolic acid, was isolated from leaves of Olea europaea by well-known two different methods, but not used for this compound before, the acidic hydrolysis method and basic acidic method. The presence of oleanolic acid was proved in both methods with qualitative and quantitative d

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Publication Date
Tue May 12 2015
Journal Name
International Journal Of Humanities, Arts, Medicine And Sciences
SYNTHESIS, SPECTRAL, DYEING PERFORMANCE AND BIOLOGICAL ACTIVITY STUDIES OF AZO DYES COMPLEXES WITH SOME METAL IONS
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Some azo compounds were prepared by coupling the diazonium salts of amines with 2,4-dimethylphenol The structure of azo compounds were determined on the basis of elemental analyses, 1HNMR, FT-IR and UV-Vis spectroscopic techniques. Complexes of nickel(II) and copper(II) have been synthesized and characterized. The composition of complexes has been established by using flame atomic absorption, (C.H.N) Analysis, FT-IR and UV-Vis spectroscopic methods as well as conductivity magnetic susceptibility measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). High molar absorbtivity of the complex solutions were observ

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Publication Date
Thu Dec 01 2011
Journal Name
Journal Of Al-nahrain University Science
Synthesis, Spectroscopic and Biological Studies of Some Metal Complexes with 2,2-Diamino–N–Phenyl Hydrazo Benzene
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Publication Date
Wed Jun 10 2015
Journal Name
Journal Of The College Of Basic Education
Synthesis, characterization and antimicrobial studies of 2-(4-antipyrine azo)-4-nitroaniline with some metal ions.
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Transition metal complexes of Co(II), Ni(II), Cu(II), and Zn(II) with 2-(4-antipyrine azo)-4-nitroaniline derived from 4-aminoantipyrine and 4-nitroaniline were synthesized. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR, UV-Vis and 1HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, the stoichiometry of the complexes has been found to be 1:2 (metal:ligand). On the basis of physicochemical data octa

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Publication Date
Wed Jan 12 2011
Journal Name
Al-mustansiriyah J. Sci
Synthesis, Spectroscopic and Biological Studies of 2-(N-Phenyl Dithio Carboxamide)Benzothiazole with some Metal Ions
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الوصف The synthesis of 2 (N-phenyl dithio carboxamid) benzothiazol Ligand (L) from reaction of 2-Mercaptobenzothiozol with phenylisothiocyanate using ratio 1: 1. The ligand was characterized by elemental analysis (CHN),'H-NMR, IR and UV-Vis. The complexes with bivalent ions (Ni, Cu, Zn, Cd and Hg) have been prepared and characterized. The structural diagnosis was established using IR, UV–Visible spectro photometer, molar conductivity, atomic absorption and molar ratio with selected metal ions (Ni2+, Cu2+). The complexes of (Ni, Cu) gave octahedral structural while the complexes of (Zn, Cd, Hg) gave tetrahedral structural. The study of biological activity of the ligand (L) and its complexes (Ni, Cu, Hg) in two deferent concentration (

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Publication Date
Sun Oct 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Investigation The Biological Activity of Some New Alkenes Based on Thiazoldin-4-one Compounds
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This work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f  from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, pos

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Publication Date
Wed Apr 01 2026
Journal Name
Journal Of Molecular Structure
Synthesis and studying the mesomorphic behavior of some new compounds based on 1H -benzimidazole-2-thiol
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Publication Date
Sun Dec 03 2017
Journal Name
Baghdad Science Journal
Network Self-Fault Management Based on Multi-Intelligent Agents and Windows Management Instrumentation (WMI)
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This paper proposed a new method for network self-fault management (NSFM) based on two technologies: intelligent agent to automate fault management tasks, and Windows Management Instrumentations (WMI) to identify the fault faster when resources are independent (different type of devices). The proposed network self-fault management reduced the load of network traffic by reducing the request and response between the server and client, which achieves less downtime for each node in state of fault occurring in the client. The performance of the proposed system is measured by three measures: efficiency, availability, and reliability. A high efficiency average is obtained depending on the faults occurred in the system which reaches to

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