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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
Tue Jan 01 2019
Journal Name
Revista De Chimie
Synthesis, Characterization and Antibacterial Activity from Mixed Ligand Complexes of 8-Hydroxyquinoline and Tributylphosphine for Some Metal Ions
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Co+2, Ni+2, Cu+2 as well Zn+2 compounds mixed ligand from 8-hydroxyquinoline(8-HQ) also tributylphosphine (PBu3) have been attended at aquatic ethyl alcohol for (1:2:2) (M:8-HQ:PBu3). Produced complexes have been identified by utilizing atomic absorption flame, FT-IR as well UV-Vis spectrum manners also magnetic susceptibility as well as conductivity methods. At addendum antibacterial efficiency from the ligands as well complexes oboist three species about bacteria have been as well examined. Ligands and their complexes show good bacterial efficiencies. Of the gained datum the octahedral geometry was proposed into whole prepared complexes

Publication Date
Fri Nov 03 2023
Journal Name
Karbala International Journal Of Modern Science
Synthesis and characterization of zirconium oxide nanoparticles using Z. officinale and S. aromaticum plant extracts for antibacterial application
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Publication Date
Sat Oct 19 2024
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Studying Thermal Analysis for Complexes of Some Metal Ions and Determining Their Activity as Antioxidants
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وفقأ للدراسات السابقة تم تحضير ليكاند آزو جديد (ن-(3-اسيتايل-2-هيدروكسي-5-مثيل-فنيل)ن-(4-كاربوكسي-سايكلوهكسيل مثيل)-ملح الدايازونيوم) وبعد التحقق من الصيغة المقترحة وفق نتائج التحاليل وبعد استخدام الليكاند لتحضير سلسلة ن المعقدات باستخدام نسب مولية متساوية (1:1) من الليكاند وتفاعلها مع كل من املاح المنغنيز والكوبلت والنيكل والنحاس والخارصين وبعد التحقق وفق تقنيات التحاليل الطيفية والتشخيصية(الاشعة فوق البنف

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Publication Date
Sun Mar 10 2013
Journal Name
Journal Of Life Sciences And Technologies
Synthesis, Characterization, and Anti-Microbial Study of Metal Complexes of Polycyclicacetal derived from PVA & Erythro-Ascorbic acid derivative
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The aim of this work is the synthesis of new grafted PVA polymer with a derivative of Erythro-ascorbic acid (pentulosono-ɣ -lactone-2, 3-enedianisoate). All synthesized compounds were characterized by thin layer chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR and mass spectra. They were also evaluated for antimicrobial properties by dilute method against four pathogenic bacteria (Escherichia coli ,Klebsiella pneumonae, Staphylococcus aureus, Staphylococcus Albus) and two fungal (Aspergillus Niger, Yeast). All polymer metal complexes showed good activities against the various microbial isolates. The polymer metal complexes showed higher activity than the free polymer. The order of increa

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Bioactivity Study of Few Metal Complexes of Curcumin with 2-(1H-Benzimidazol-2-yl) Aniline
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We have synthesized many metal (II) complexes using curcumin L1 as the major ligand and 2-(1H-Benzimidazol-2-yl) aniline L2 as a supporting ligand. The complexes were characterized by spectroscopy methods such as; molar conductivity, elements microanalysis, Fourier-transform spectroscopy (FT-IR), UV-vis, and mass spectroscopy. Both curcumin ligands and L2 were found to be capable of binding to M(II) and metal ions via their two N atoms, according to the data. The formula for the complexes is the same. [M (L1)(L2)H2OCl], where M is Ni(II), Co(II), Cu(II), Cd(II), and Hg(II) (II). Octahedral complexes are proposed for the prepared compounds. The bio-actives suggested that the complexes are effective against bacteria and fungus on a mi

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Publication Date
Fri Jun 28 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases
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Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted o

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some Novel Oxazine, Thiazine and Pyrazol Derivatives
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In this paper, some chalcone derivatives (C1, C2) were synthesized based on the reaction of equal amount of substituted acetophenone and substituted banzaldehyde in basic medium. Oxazine and thiazine derivatives were prepared from the reaction of chalcones (C1-C2) with urea and thiourea respectively in a basic medium. Pyrazole derivatives were prepared based on the reaction of chalcones with hydrazine mono hydrate or phenyl hydrazine in the presence of glacial acetic acid as a catalyst. The new synthesized compounds were identified using various physical techniques like1 H-NMR and FT-IR spectra.

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Publication Date
Mon Aug 10 2009
Journal Name
European Journal Of Scientific Research
Synthesis and characterization and Fungicidal Activity of Triorganotin(IV) with Benzamidomethionine
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Publication Date
Tue Oct 22 2019
Journal Name
Scientia Pharmaceutica
Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group
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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenoc

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Publication Date
Mon Dec 28 2020
Journal Name
The Iraqi Journal Of Veterinary Medicine
Synthesis and Characterization of Black Currant Selenium Nanoparticles (Part I)
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The present study aimed to synthesize selenium nanoparticles (SeNPs) using aqueous extract of black currant as a reducing agent. The green synthesized black currant selenium nanoparticles (BCSeNPs) were identified by color change. The characterization of SeNPs was achieved by Ultraviolet-visible (UV–VIS) spectroscopy, scanning electron microscopy (SEM), X–ray diffraction analysis (XRD), and Fourier transform infrared spectroscopy (FTIR). These tests were used to detect: stability, morphology, size, crystalline nature, and functional groups present on the surface of BCSeNPs. The results revealed appearance of the brick-red color indicating the specific color of selenium nanoparticles, and UV-Vis spectroscopy showed band absorbanc

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