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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
Thu Oct 03 2024
Journal Name
Applied Organometallic Chemistry
Synthesis, Characterization, Molecular Docking, Cytotoxicity, and Antimicrobial Activity of Schiff Base Ligand and Its Metal Complexes
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ABSTRACT<p>A Schiff base ligand (L) was synthesized via condensation of <italic>N</italic>‐(1‐naphthyl)ethylenediamine dihydrochloride with phthalaldehyde. The ligand was characterized by FT‐IR, UV–Vis, <sup>1</sup>H NMR, mass spectrometry, and elemental analysis (C, H, N). Five metal complexes (Co(II), Ni(II), Cu(II), Zn(II), and Cd(II)) were prepared with the ligand in a 1:1 (M:L) ratio using an aqueous ethanol solution. The complexes were characterized by FT‐IR, UV–Vis, mass spectrometry, and elemental analysis (C, H, N). Additionally, <sup>1</sup>H NMR spectroscopy was employed for Cd(II) complex. Antimicrobial activity of the ligand and its metal complexes against </p> ... Show More
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Publication Date
Thu Oct 03 2024
Journal Name
Applied Organometallic Chemistry
Synthesis, Characterization, Molecular Docking, Cytotoxicity, and Antimicrobial Activity of Schiff Base Ligand and Its Metal Complexes
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ABSTRACT<p>A Schiff base ligand (L) was synthesized via condensation of <italic>N</italic>‐(1‐naphthyl)ethylenediamine dihydrochloride with phthalaldehyde. The ligand was characterized by FT‐IR, UV–Vis, <sup>1</sup>H NMR, mass spectrometry, and elemental analysis (C, H, N). Five metal complexes (Co(II), Ni(II), Cu(II), Zn(II), and Cd(II)) were prepared with the ligand in a 1:1 (M:L) ratio using an aqueous ethanol solution. The complexes were characterized by FT‐IR, UV–Vis, mass spectrometry, and elemental analysis (C, H, N). Additionally, <sup>1</sup>H NMR spectroscopy was employed for Cd(II) complex. Antimicrobial activity of the ligand and its metal complexes against </p> ... Show More
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Publication Date
Wed Aug 13 2025
Journal Name
Molecular Crystals And Liquid Crystals
Synthesis, characterization and mesomorphic behavior of twin pyrazole ligands and their metal complexes containing dithiocarbamat units
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Publication Date
Thu Apr 25 2019
Journal Name
Engineering And Technology Journal
Synthesis, Characterization and Antibacterial activities of Uracil and Uracil–Oxalate Complexes with Cr(III) and Fe(III)
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New complexes of the some trivalent transition metal ions of the uracil such as [M(Ura)3Cl3] and mixed ligand metal complexes with uracil and oxalic acid [M(Ura)2(OA)(OH2)Cl].H2O type, where (Ura)=Uracil, (OA= Oxalic acid dihydrate, (M= Cr+3 and Fe+3) were synthesized and characterized by the elemental analysis, FT.IR, electronic spectra, mass spectra and magnetic susceptibility as well as the conductivity measurements. Six–coordinated metal complexes were suggested for the isolated complexes of Cr+3 and Fe+3 with molecular formulas dependent on the nature of uracil and oxalic acid present. The proposed molecular structure for all complexes with their ions is octahedral geometries. The antibacterial efficiency was tested of metal salts, l

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Publication Date
Wed Sep 08 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis And Characterization Of Metal(II) Complexes With Azo Dye Ligand And Their Industrial And Biological Applications
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Azo ligand 4-((2-hydroxy-3,5-dimethylphenyl)diazenyl) benzoic acid was synthesized from 4-aminobenzoic acid and 2,4- dimethylphenol. Azo dye compounds have been characterized by different techniques (1H-NMR, UV-Vis and FT-IR). Metal chelates of (ZnII, CdII and HgII) have been synthesized with azo ligand (L). Produced compounds have been identified by using spectral studies, elemental analysis(C.H.N.) and conductivity. Produced metal chelates were studied using mole ratio as well sequences contrast types. Rate of concentration(1×10-4-3×10-4 Mole/L) sequence Beer's law. Compound solutions have been noticed height molar absorptivity. The addendum of ligand and compounds has applied as disperse dyes on cotton fabrics for antibacterial activit

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Publication Date
Tue Dec 31 2019
Journal Name
Journal Of Engineering And Applied Sciences
Design and Implementation of Electronic Infrastructure for Academic Establishment
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Publication Date
Tue Jan 01 2019
Journal Name
Journal Of Cosmetics, Dermatological Sciences And Applications
A New Regimen in the Treatment of Psoriasis Using Oral Methotrexate
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Publication Date
Mon Sep 30 2013
Journal Name
Iraqi Journal Of Science
Protective Effect of Vitamin A against Oxidative Stress Caused by Methotrexate
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Methotrexate (MTX), a folate antagonist agent, is mainly used in treatment of malignant tumors and autoimmune diseases. The present study was undertaken to determine whether antioxidant vitamin (vitamin A) could ameliorate methotrexate induced oxidative stress in male rabbits. Twenty male rabbits were randomly assigned into four groups. Group 1: control group, Group 2: MTX-treated group (received 20 mg/kg MTX intraperitoneally), Group 3: Vit.A treated group received 5000 IU Vit.A orally) and Group 4: MTX+Vit.A treated group received MTX 20 mg/kg plus 5000 IU vit.A). After 4 weeks of treatment, blood samples were collected by cardiac puncture to determine the serum malondialdehyde (MDA), as a good indicator for lipid peroxidation and

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Vitamin D3 on Methotrexate- Induced Jejunum Damage in Rats
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Both methotrexate and vitamin D3 are used in combination for the treatment of various diseases. The aim of this study is to highlight the effect of vitamin D3 on methotrexate-induced jejunum damage using biochemical and   histopathological  studies. Seven groups of both sexes of rats were selected and treated as follows: (Group I and Group II) : control 1,control 2 (I.P normal saline) daily for 14 and 21 days respectively ; (Group III and Group IV) :vitamin D3 groups (500 IU/rat/day) orally for 14 and 21 days, respectively;(Group V): once daily dose of methotrexate 20mg/kg, I.P injected for 4 days;(Group VI):vitamin D3 (500 IU/rat/day) once daily for 14 days and methotrexate (20 mg/kg I.P) injected only at day 10;.(Group

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Publication Date
Sat Oct 01 2016
Journal Name
World Journal Of Pharmaceutical Research
TERATOGENIC EFFECT OF METHOTREXATE ON HISTOGENESIS OF TESTIS IN NEWBORN RAT
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Background: Methotrexate (MTX) was one of the first drugs synthesized for a specific chemotherapeutic purpose used to inhibit folic acid (FA) for the treatment of acute lymphoblastic leukemia in children. Its history is closely related to the discovery and characterization of folic acid. It is used clinically in medicine to treat a range of cancerous and noncancerous conditions. MTX is currently used in gynecology to treat disorders arising from trophoblastic tissue, namely, ectopic pregnancy. MTX, the most frequently used diseasemodifying anti-rheumatic drug (DMARD), suppresses disease activity and reduces joint damage. The aim of study: It is designed to demonstrate the effect of MTX (7.5 mg/wk.) on the histogenesis of gonad (testis) of n

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