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Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple  drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed  towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of  two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis  of the target compounds was  accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed  that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug  selectively  into the cancer cells to be hydrolyzed by enzymes that are elevated in  tumor tissues compared with normal tissues . Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.

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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
Sun Oct 30 2022
Journal Name
Iraqi Journal Of Science
Synthesis of a Series of α, β-Unsaturated Ketoximes and their Corresponding Acetate Esters
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      A series of 1,3-diarylprop-2-en-1-one oximes (7-12) were synthesized via reaction of 1,3-diarylprop-2-en-1-one (1-6) with NH2OH. HCl in dry pyridine. In order to produce the required products (13-18) as anti-isomers, these products (7–12) were then treated with acetic anhydride in dry pyridine. Different substitutes are maintained, resulting in the separation of different products in different yields The recently produced esters are thought to be useful as building blocks for the synthesis of substituted pyridines and many other nitrogen-holding complexes, which are elaborate structures in medicinal chemistry and present in a variety of pharmaceutical medications. The synthesized products were characteriz

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Publication Date
Sat Jun 27 2020
Journal Name
Iraqi Journal Of Science
Green Synthesis Concept of Nanoparticles From Environmental Bacteria and Their Effects on Pathogenic Bacteria
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Soil bacteria play an interesting role in the reduction of Ag+ ions and the formation of silver nanoparticles (AgNPs), which may be a good source for nanoparticles and play a major role in nanotechnology applications. The concept of this project was to study the effects of these environmentally produced nanoparticles on the growth of some pathogenic bacteria. The environmental bacteria were isolated from soil, purified on broth cultures, and centrifuged, while the supernatant was extracted to detect its ability to convert silver nitrate to nanoparticles. The AgNPs was detected by Atomic Force Microscopy (AFM), while Granularity Cumulating Distribution (GCD) was employed to estimate the AgNPs sizes. The results showed the

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Publication Date
Mon Nov 29 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Antibacterial Screening of New Schiff Bases Based on N-(4-acetophenyl) Succinimide
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A series of nine new Schiff bases based on N-(4-acetophenyl)succinimide were synthesized via multistep synthesis. In the first step N-(4-acetophenyl)succinamic acid was prepared via reaction of succinic anhydride with 4-aminoacetophenone. The prepared amic acid was dehydrated in the second step producing N-(4-acetophenyl)succinimide. The prepared succinimide represents a modified methyl ketone bearing succinimde cycle and ready for introducing in condensation reaction thus in the third step the prepared imide was introduced in acid-catalyzed condensation reaction with a variety of primary aromatic amines affording the new target Schiff bases. The results of antibacterial screening of the newly synthesized Schiff bases indicated that they

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Publication Date
Mon Jul 20 2020
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antibacterial Activity of PEG Polycyclic Acetal Metal Complex/ PVA Polymer Blend Film
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     Polyacetal was synthesized from the reaction of Polyethylene glycol with4- dimethylaminobenzaldehyde.Polymer metal complex was synthesized by the reaction with Ag+; polymer blend with polyvinyl alcohol was synthesized solution casting technique. All synthesized compounds were characterized by FT-IR in addition to the antimicrobial activity. The FT-IR spectra indicate the formation of the polyacetal. The DSC resultsindicatethe thermal stability regarding the synthesized polymer blends. The synthesized polyacetal, its metal complex and PA blend against four types of bacteria (gram+ve) Staphylococcus aureas, Bacillus subtilis and (gram –ve)Klebsiella pneumoniae, Escherichia Coli w

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Publication Date
Wed Jul 10 2024
Journal Name
Pharmacia
Molecular docking, ADMET, synthesis and evaluation of new indomethacin hydrazide derivatives as antibacterial agents
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Bacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used

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Publication Date
Thu Nov 01 2018
Journal Name
Colloids And Surfaces B: Biointerfaces
Green synthesis of silver nanoparticles using turmeric extracts and investigation of their antibacterial activities
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Publication Date
Mon May 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Organic Synthesis of Some New Compounds Derived from Furfural and Their Evaluation as Antioxidants
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Heterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep

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Publication Date
Sun Jan 01 2023
Journal Name
Dental Hypotheses
Revolutionizing Systematic Reviews and Meta-analyses: The Role of Artificial Intelligence in Evidence Synthesis
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Publication Date
Sun Dec 16 2012
Journal Name
Journal Of Physical Education
Analysis study for some offensive plans for Iraqi Duhok participated in Asian club in Basketball 2011
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The tactical side in application of offensive plans in basketball did not take a large in scientific research because it always change because it related in mental ability of players and for the condition of the game and researchers notice that from their followed a lot of games for Duhok basketball club in Iraq league. There is a problem that connected in games results it clears in weakness in application of offensive plans in all kind (man to man & zone defense & side ball plans & under basketball and half court). The goal of study concentrate by designing a sheet for som offensive plans for study and analysis to Duhok club on Asian Championship 2011 at the base the sample contained (Iraq Duhok & application science Jordan & Lebanon sport

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