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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 Feb 28 2023
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis and Characterization of Molecularly Imprinted Polymers for Metronidazole by using Allyl Chloride and Allyl Bromide as Monomers
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Metronidazole-MIPs were prepared by using (MDZ) as the template as well as allylchloride (AYC) or allylbromide (AYB) as monomer, used (TMPTA) tri-methylol propane tri-acrylate or ethylene glycol di-methyl acrylate (EGDMA) as cross-linker and initiator used (BP) benzyl peroxide. By using different plasticizers (di butyl Phthalate (DBPH), Nitrobenzene (NB), oleic acid (OA) and paraffin) for MDZ-MIP1 and (Di-butyl sebecate (DBS), Di-methyl acrylate (DMA), Tributylphosphate(TBP) and Tris(ethylhexyl phosphate (TEHP) ) for MDZ-MIP2. Membranes of MIPs were prepared in PVC matrix. The characterizations of each electrode were determined The Slope range from (55.083 - 43.711) mV/decade, Limit of Detection (8 X 10 -4- 2 X 10-6) and Linearity

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Publication Date
Thu Oct 06 2022
Journal Name
Pakistan Journal Of Medical & Health Sciences
Synthesis, Characterization, and Biological Activity of Mixed ligand Complexes from 8-Hydroxyquinoline and new Ligand for β-Enaminone
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The synthesized ligand [4-chloro-5-(N-(5,5-dimethyl-3-oxocyclohex-1-en-1-yl)sulfamoyl)-2-((furan-2-ylmethyl)amino)benzoic acid] (H2L1) was identified utilizing Fourier transform infrared spectroscopy (FT-IR), 1 H, 13 C – NMR, (C.H.N), Mass spectra, UVVis methods based on spectroscopy. To detect mixed ligand complexes, analytical and spectroscopic approaches such as micro-analysis, conductance, UV-Visible, magnetic susceptibility, and FT-IR spectra were utilized. Its mixed ligand complexes [M(L1)(Q)Cl2] [ where M= Co(II), Ni(II) , and Cd(II)] and complexes [Pd(L1)(Q)] and [Pt(L1)(Q)Cl2]; [H2L1] =β-enaminone ligand =L1 and Q= 8-Hydroxyquinoline = L2]. The results showed that the complexes were synthesised utilizing the molar ratio M: L1

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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
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
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
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effect of Silibinin in Lowering the Intraocular Pressure in Normotensive Rabbits: Interaction with Pilocarpine and Cyclopentolate
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Previous data indicated the effectiveness of silibinin as intraocular pressure (IOP) - lowering agent.  The present study was performed to evaluate the interaction of silibinin with pilocarpine or cyclopentolate in lowering IOP in normotensive rabbits. The effects of topically instilled silibinin hemisuccinate solution (0.75%) alone or adjunctly combined with 2% pilocarpine or 1% cyclopentolate on the IOP of normotensive rabbits were evaluated using indentation tonometry. The results showed that 0.75% solution of silibinin was found more potent than pilocarpine (2% drops) in lowering IOP of normotensive rabbits, while their combination results in longer duration of action. Moreover, the elevated IOP values produced by cyclopentolate

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Publication Date
Tue Mar 06 2007
Journal Name
Iraqi J Pharm Sci,
Effect of Silibinin in Lowering the Intraocular Pressure in Normotensive Rabbits: Interaction with Pilocarpine and Cyclopentolate
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Previous data indicated the effectiveness of silibinin as intraocular pressure (IOP) - lowering agent. The present study was performed to evaluate the interaction of silibinin with pilocarpine or cyclopentolate in lowering IOP in normotensive rabbits. The effects of topically instilled silibinin hemisuccinate solution (0.75%) alone or adjunctly combined with 2% pilocarpine or 1% cyclopentolate on the IOP of normotensive rabbits were evaluated using indentation tonometry. The results showed that 0.75% solution of silibinin was found more potent than pilocarpine (2% drops) in lowering IOP of normotensive rabbits, while their combination results in longer duration of action. Moreover, the elevated IOP values produced by cyclopentolate (1%drops

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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 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
Sun Jul 23 2023
Journal Name
University Of Samarra
Synthesis, spectral characterization and thermal ‎study of complexes of ions of some metallic ‎elements with new cyclic ligands
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The purpose of my thesis is to prepare four new ligands (L1-L4) that have been ‎used to prepare a series of metal complexes by reacting them with metal ions:‎ ‎ M=(Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II) ‎ ‎ Where succinyl chloride was used as a raw material for the preparation of ‎bi-dented ligands (L1-L4) by reacting it with potassium thiocyanate as a first ‎step and then reacting with (2-aminobenzothiazole, Benzylamine, 4-‎aminoantipyrine, Sulfamethoxazole) respectively as a second step with the use ‎of dry acetone as a solvent, the chemical formula of the four ligands prepared in ‎succession:‎ N1,N4-bis(benzo[d]thiazol-2-ylcarbamothioyl)succinamide (L1)‎ N1,N4-bis(benzylcarbamothioyl)succinami

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