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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 Feb 06 2023
Journal Name
Journal Of The College Of Basic Education
Synthesis and Characterization of some biologically active transition metal complexes for a ligand derived from dimedone with mixed ligands.
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The aim of the work is synthesis and characterization of bidentate ligand [3-(3-acetylphenylamino)-5,5-dimethylcyclohex-3-enone][HL], from the reaction of dimedone with 3-amino acetophenone to produce the ligand [HL], the reaction was carried out in dry benzene as a solvent under reflux. The prepared ligand [HL] was characterized by FT-IR, UV-Vis spectroscopy, 'H, 8C-NMR spectra, Mass spectra, (C.H.N) and melting point. The mixed ligand complexes were prepared from ligand [HL] was used as a primary ligand while 8-hydroxy quinoline [HQ] was used as a secondary ligand with metal ion M(IT).Where M(IT) = (Mn ,Co ,Ni ,Cu ,Zn ,Cd and Pd) at reflux ,using ethanol as a solvent, KOH as a

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Publication Date
Thu Feb 20 2025
Journal Name
Experimental Oncology
The Potential Role of HDAC1 and HDAC3 Immunoexpression in P53 Downregulation and Tumor Aggressiveness of Colon and Rectum Carcinomas Patients
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Background. Colorectal cancer, ranking second place in global cancer mortality, arises from diverse causes. There is growing recognition of the substantial involvement of the epigenetic modifications of histones at the DNA level in the occurrence of CRC. Aim. To assess the expression of p53, HDAC1, and HDAC3 proteins in a cohort of CRC patients and to analyze potential relationship between their expression and the stages of CRC progression. Materials and Methods. The retrospective investigation was carried out on 95 paraffin-embedded CRC tissue samples. The expression of p53, HDAC1, and HDAC3 was assessed immunohistochemically. Results. Notably, the expression of the p53 protein in CRC tissue samples exhibited a prominent correlatio

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Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Synthesis , characterization and biological activity study of N-substituted sulfonamido maleimides substituted with different heterocycles
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Eighteen new cyclic imides (maleimides) conncted to benzothiazole moiety through sulfonamide group were synthesized via multistep synthesis.The first step involved preparation of two maleamic acids N-phenylmaleamic acid and N-benzylmaleamic acid via reaction of maleic anhydride with aniline or benzyl amine.Dehydration of the prepared amic acids by treatment with acetic anhydride and anhydrous sodium acetate in the second step afforded N-phenylmaleimide and N- benzyl maleimide which in turn were treated with chlorosulfonic acid in the third step to afford 4-(N-maleimidyl) phenyl sulfonyl chloride and 4-(N-maleimidyl) benzyl sulfonyl chloride respectively.In the Fourth step of this work each one of the two prepared maleimidyl sulfonyl chlorid

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Publication Date
Mon Mar 11 2019
Journal Name
Baghdad Science Journal
A Spectral, Optical, Microscopic Study, Synthesis and Characterization of PVC Films Containing Schiff Base Complexes
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In this work, synthesis of conducting polymeric films namely, PVC thin films was carried out containing Schiff base (L) with Cu2+, Cr3+, Ni2+, Co2+, in addition to inspecting the possibilities of measuring energy gap values of PVC-L-M with variety metal ions. These new polymeric films (PVC-L-M) were characterized by FTIR spectrophotometry, energy gap and surface morphology. The optical data recorded that the band gap values are influenced by the type of metals. All modified films have a red shift in optical properties in the ultraviolet region. The PVC-L-Co(II) was the lowest value of the optical band gap, 3.1 eV.

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Publication Date
Wed Aug 26 2020
Journal Name
Iraqi Journal Of Agricultural Sciences
ECO-FRIENLY SYNTHESIS OF GOLD NANOPARTICLES AND STUDY THEIR EFFECT WITH ANTIBIOTICS AGAINST ACINETOBACTER BAUMANNII
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This study was aimed to produce AuNPs biologically using Klebsiella pneumoniae and study their synergistic effect with some antibiotics.Technologies of nanoparticles are quick and are employed in many applications in biomedicine. The potential of metallic nanoparticle as an anti-microbial agent is greatly investigated which considered as an alternative method to reduce the challenges of multi-drug resistance microbes. The present study discusses the novel approach to synthesize nanoparticles involving eco-friendly synthesis of gold nanoparticles using Klebsiella pneumoniae and study their effect as antimicrobial spectrum .Also study synergism effect of gold nanoparticles with antibiotic against Acinetobacter baumannii. These approac

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Publication Date
Sat May 30 2020
Journal Name
Neuroquantology
Synthesis and Study NiO Charactrization of Extract from Green Tea Plant Prepared by Chemical Method
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Publication Date
Thu Feb 28 2019
Journal Name
Journal Of Engineering
Hydraulic Analysis and Performance Evaluation of Combined Trunk Sewers: A Case Study of Baghdad City.
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Sewer system plays an indispensable task in urban cities by protecting public health and the environment. The operation, maintenance, and rehabilitation of this network have to be in a sustainable and scientific manner. For this purpose, it is important to support operators, decision makers and municipalities with performance evaluation procedure that is based on operational factors. In this paper, serviceability and performance indicator (PI) principles are employed to propose methodology comprising two enhanced PI curves that can be used to evaluate the individual sewers depending on operational factors such as flowing velocity and wastewater level in the sewers. In order to test this methodology; a case study of al-Ru

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Publication Date
Tue Oct 01 2019
Journal Name
Journal Of Engineering
Hydraulic Analysis and Performance Evaluation of Combined Trunk Sewers: a Case Study of Baghdad City.
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Sewer system plays an essential task in urban cities by protecting public health and the environment. The operation, maintenance, and rehabilitation of this network have to be sustainable and scientifically. For this purpose, it is crucial to support operators, decision makers and municipalities with performance evaluation procedure that is based on operational factors. In this paper, serviceability and performance indicator (PI) principles are employed to propose methodology comprising two enhanced PI curves that can be used to evaluate the individual sewers depending on operational factors such as flowing velocity and wastewater level in the sewers. To test this methodology; a case study of al-Rusafa in Baghdad city is

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Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and Spectroscopic Study of 3-Hydroxy-2-(3-(4- Nitrobenzoyl) Thiouriedo) Propanoic Acid with their Metal Complexes
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A new ligand 3-hydroxy-2-(3-(4-nitrobenzoyl) thiouriedo) propanoic acid (NTP) where synthesized by reaction of 4-nitro benzoyl isothiocyanate with serine amino acid. The ligand was characterized by FT-IR, NMR spectra and the elemental analysis. The transition metal complexes of this ligand where synthesize and characterized by UV-Visible spectra, FT-IR, magnetic suscpility, conductively measurement, The general formula [M (NTP) 2] where M+2= (Mn, Co, Ni, Cu, Zn, Cd, Hg,), the form of molecular for these complexes as tetrahedral except Cu has square planer.

Publication Date
Thu Jun 02 2016
Journal Name
Alustath Journal For Human And Social Sciences
Islamic Electronic Libraries and The service for downloading Research and Comic books (PDF): An Evaluation study
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The research aims to evaluate Islamic electronic libraries and their service for downloading research and illustrated books, explaining their origins, features and types. The research was limited to the libraries available on the Internet that provide the service for downloading research and illustrated books. The researcher relied on the survey approach to identify the libraries and a sample of them (20 libraries) was selected. For the purpose of evaluating it according to five criteria related to the preparation and publication of Islamic electronic libraries (the responsible party, the goals and objectives, the year, the services it provides, the sections and subject specializations of its contents) and five criteria related to the servi

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