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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
Wed Jan 01 2025
Journal Name
Medical Journal Of Babylon
Optimum Conditions for Pyomelanin Production and Characterization from Local Isolates of Pseudomonas aeruginosa
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Nowadays, there is increased interest in the biosynthesis of microbial melanin related to their numerous biological functions and applications in many fields, especially in medical fields, including immune-modulating, antimicrobial antibiotic, antiviral antivenin, anticancer, antitumor activity, and anti-biofilm activity. Pyomelanin is a hydrophobic macromolecule that is typically dark brown or black in color, formed by the oxidative polymerization of phenolic or indolic compounds. Pyomelanin is reported to be safe for consumption, thus providing a crucial strategy for biocontrol of biofilm. Furthermore, natural pyomelanin is known as a potent antioxidant, photoprotective, and free radical scavenging. Objective: This study focuses on the

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility
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Abstract

            Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis,  and for the prophylaxis of fungal infections in immunocompromised patients.

           The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.

          Itraconazole nanosuspension was produced by a

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Publication Date
Tue Aug 06 2024
Journal Name
Fullerenes, Nanotubes And Carbon Nanostructures
Preparation and characterization of PVA/MWCNT nanocomposites: a composition dependence study of structural, optical and mechanical properties
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Publication Date
Tue Aug 06 2024
Journal Name
Fullerenes, Nanotubes And Carbon Nanostructures
Preparation and characterization of PVA/MWCNT nanocomposites: a composition dependence study of structural, optical and mechanical properties
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This work investigates the properties of polyvinyl alcohol (PVA) nanocomposite films with varying multi-walled carbon nanotube (MWCNT) content, ranging from 2 to 8 wt.%. The films were prepared using a solution casting method and characterized using UV-visible spectroscopy, optical microscopy, X-ray diffraction, and tensile tests. The prepared PVA/MWCNT nanocomposite films exhibited optical band gap values ranging from 3.5 eV to 5.3 eV. XRD analysis confirmed the semi-crystalline nature of these nanocomposites. Mechanical properties, including hardness, yield strength, ultimate tensile strength, and Young's modulus, were enhanced by increasing MWCNT content by up to 8%. Contact angle measurements showed an increase in hydrophobicity with in

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Publication Date
Tue Mar 31 2026
Journal Name
Aip Conference Proceedings
Synthesis, identification of some new oxazolidinone and thiazolidinone derivatives and study anti-oxidant and anti-microbials activity
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In this study, new oxazolidinone and thiazolidinone derivatives were synthesized through a three-step process. In the first step, o-aminothiophenol was reacted with p-aminobenzoic acid in hydrochloric acid to produce an amine containing a thiazole ring, achieving a product yield of 80%. The second step involves synthesizing Schiff bases (E1-E4) by reacting 4-(benzo[d]thiazol-2-yl)aniline with various aromatic aldehydes in the presence of glacial acetic acid. This reaction yields products of 76% to 90%. In the third step, the Schiff derivatives (E1-E4) are reacted with glycolic acid and thioglycolic acid to obtain the desired products. Oxazolidinone derivatives (N1-T1) were produced with rates ranging from 66% to 74%, while thiazolidin

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Publication Date
Thu Nov 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
The Impact of Technological Change in Process Design Decisions (Applied study in an organization)
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Abstract:

     Due to the importance of technology and the accompanying changes of the environment affecting companies that use the technology mainly in their work, especially as most companies live in an unstable dynamic environment, which motivated the researchers to choose the International Company for smart card (Keycard) as a field of research and find ways to them to face Those changes.

     The problem of the study was "limited attention to the components of technological change", which included research and development, innovation and information technology, which had an impact on the design decisions of the process (process selection, cust

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Publication Date
Tue Jan 01 2019
Journal Name
Energy Procedia
Synthesis and Study the Structure, electrical and optical properties of Bi2-xCdxSr2Ca2Cu3O10+ δ thin film Superconductors
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Publication Date
Tue Jul 01 2008
Journal Name
D
Synthesis and Identification of Some New Derivatives of Schiff bases Compounds and study their Biological activity
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A new series of Schiff bases compounds , containing an azomethine linkage was synthesized and expected to be biologically active .The structures of these compounds were identified by IR , Uv/vis spectra , melting points and followed by T.L.C.The biological activity of these compounds was studied

Publication Date
Sun Dec 06 2015
Journal Name
Baghdad Science Journal
Synthesis and characterization of some biological active transition metal complexes of Schiff base derived from cefixime with mixed ligand 8-hydroxy quinoline
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The aim of the work is synthesis and characterization of bidentate ligand [dipotassium sodium7-((E)-2-(2-((Z)-1-carboxylatoethylideneamino)thiazol-4-yl)-2 (carboxylatemethoxyimino) acet amido)-8-oxo-3-vinyl-5- thia-1-azabicyclo[4.2.0] oct-2- ene-2- carboxylate] [Nak2L], from the reaction of cefixime with sodium pyruvet to produce the ligand [Nak2L], the reaction was carried out in methanol as a solvent under reflux. The prepared ligand [Nak2L] which was characterized by FT-IR, UV-Vis spectroscopy, 1H, 13C-NMR spectra, Mass spectra, (C.H.N) and melting point. The mixed ligand complexes were prepared from ligand [Nak2L] was used as a primary ligand while 8-hydroxy quinoline [Q] was used as a secondary ligand with metal ion M(Π).Where

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Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Synthesis, Characterization, and Biological Activity of New Metal Ion Complexes with Schiff Base (Z)-3((E)-2-Hydroxybenzylidene) Hydrazineylidene) Indolin-2-One
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The study involved preparing a new compound by combining between 2-hydroxybenzaldehyde and (Z)-3-hydrazineylideneindolin-2-one resulting in Schiff bases and metal ions: Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) forming stable minerals-based-Schiff complexes. The formation of resulting Schiff bases is detected spectrally using LC-Mss which gave corresponding results with theoretical results, 1H-NMR proves the founding of N=CH signal, FT-IR indicates the occurrence of imine band and UV-VIs mean is proved the ligand formation. On the other hand, minerals-based-Schiff was characterized using the same spectral means that relied with ligand (Schiff bases). Those means gave satisfactory results and proved the suggested distinguishable geometries.

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