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.
In this study, synthesis of polymer Nanocomposites through the blending of prepared polymers with polyvinyl alcohol (a synthetic polymer) or chitosan (a natural polymer) then mixed with nano oxide silica by many steps. The new compound [I] was obtained via reaction of 3,3’-dimethoxybiphenyl-4,4’-diamine as starting material with malic anhydride in DMF then treatment with ammonium persulfate (NH4 )2 S2 O8 (as the initiator) in order to produce polymer [II]. Also, we prepared new polymers [III-V] by using the same starting material (3,3’-dimethoxybiphenyl-4,4’-diamine) with glutaric acid or adipic acid or isophthalic acid in DMF and pyridine. In this study, new polymer blending [VI-IX] and [X-XIII] were synthesized from a prepared pol
... Show MoreThis paper describes the synthesis of ?- Fe2O3 nanoparticles by sol-gel route using carboxylic acid(2-hydroxy benzoic acid) as gelatin media and its photo activity for degradation of cibacron red dye . Hematite samples are synthesized at different temperatures: 400, 500, 600, 700, 800 and 900 ?C at 700 ?C the ?-Fe2O3 nanoparticles are formed with particle size 71.93 nm. The nanoparticles are characterized by XRD , SEM, AFM and FTIR . The 0.046 g /l of the catalyst sample shows high photo activity at 3x10-5M dye concentration in acidic medium at pH 3.
By unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.
1-(4-amino-3-(benzo[d]thiazol-2-yldiazenyl)phenyl)ethanone has been synthezied by reaction the diazonium salt of 2-aminobenzothiazole with 4-aminoacetophenone. Specroscopic studies ( FTIR,UV-Vis, 1H and 13CNMR) and microelemental analysis (C.H.N.S.O) are use to identified of the azo ligand. Metal chelates of some transition metals were performed as well depicted. Complexes were identified using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4 - 3×10-4 mol/L). height molar absorbtivity of compoun
... Show MoreAzo-Schiff base compounds (L1 and L2) have been synthesized from the reaction of m-hydroxy benzoic acid with 1,5-dimethyl-3-[2-(5-methyl-1H-indol-3-yl)-ethylimino]-2-phenyl-2,3- dihydro-1H-pyrazol-4-ylamine and with 3-[2-(1H-indol-3-yl)-ethylimino]-1,5-dimethyl-2-phenyl- 2,3-dihydro-1H-pyrazol-4-ylamine. The free ligands and their complexes were characterized based on elemental analysis, determination of metal, molar conductivity, (1H, 13C) NMR, UV–vis, FT-IR, mass spectra and thermal analysis (TGA). The molar conductance data revealed that all the complexes are non-electrolytes. The study of complex formation via molar ratio in DMF solution has been investigated and results were consistent to those found in the solid complexes with a rat
... Show MoreThe flavonoglycone hesperidin is recognized as a potent anti-inflammatory, anticancer, and antioxidant agent. However, its poor bioavailability is a crucial bottleneck regarding its therapeutic activity. Gold nanoparticles are widely used in drug delivery because of its unique properties that differ from bulk metal. Hesperidin loaded gold nanoparticles were successfully prepared to enhance its stability and bioactive potential, as well as to minimize the problems associated with its absorption. The free radical scavenging activities of hesperidin, gold nanoparticles, and hesperidin loaded gold nanoparticles were compared with that of Vitamin C and subsequently evaluated in vitro using 2,2-diphenyl-1-picrylhydrazyl assay. The antioxi
... Show MoreThis study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s
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