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.
Orthogonal Frequency Division Multiplexing (OFDM) is an efficient multi-carrier technique.The core operation in the OFDM systems is the FFT/IFFT unit that requires a large amount of hardware resources and processing delay. The developments in implementation techniques likes Field Programmable Gate Array (FPGA) technologies have made OFDM a feasible option. The goal of this paper is to design and implement an OFDM transmitter based on Altera FPGA using Quartus software. The proposed transmitter is carried out to simplify the Fourier transform calculation by using decoder instead of multipliers. After programming ALTERA DE2 FPGA kit with implemented project, several practical tests have been done starting from monitoring all the results of
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Experimental work from Magnetic Abrasive Finishing (MAF) tests was carried out design parameters (amplitude, and number of cycle which are formed the shape of electromagnetic pole), and technological parameters (current, cutting speed, working gap, and finishing time) all have an influence on the mechanical properties of the surface layer in MAF process. This research has made to study the effect of design and technological parameters on the surface roughness (Ra), micro hardness (Hv) and material removal (MR) in working zone. A set of experimental tests has been planned using response surface methodology according to Taguchi matrix (36) with three levels and six factors
... Show MoreIn light of the intellectual and technological progress within the current developments of time, as well as the emergence of digital tools and means of display and communication, which had a major role in the shifts of the time of globalization in various commercial and economic fields, as well as areas of transferring the design image and its stages of development to customers and the convergence of views between the customer and the interior designer, which are the most important pillars of the design process As a whole, and accordingly, there is an urgent need for a process of intellectual balance between them through digital tools from the technical side and through social media from the intellectual side. Customer comments via socia
... Show MoreWe can understand interior design as a series of interconnected human principles and goals formed by science and knowledge to build a human product that reveals or gives meaning to things، and this can be presented through ecology as a system concerned with environmental aspects and as part of interior design، seeking to achieve aesthetic and functional values، in an interactive form between spaces The interior and its occupants are within an environmental balance full of life، and the ecological interior design attaches great importance to the embodiment of spiritual aspects in the internal environment، in addition to emphasizing the importance of protecting the environment and preserving resources through saving in its use and usi
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In this study, the effect of carboxylic methyl cellulose (CMC), and sodium dodcyl benzene sulfonate (SDBS) as an aqueous solution on the drag reduction was investigated. Different concentrations of (CMC) and (SDBS) such as (50, 100, 150, 200, 250, 300, 350, 400, 450, and 500 ppm) were used to analyze the aqueous solution properties, including surface tension, conductivity, and shear viscosity. The optimum four concentrations (i.e., 50, 100, 200, and 300 ppm) of fluid properties were utilized to find their effect on the drag reduction. Two different PVC pipe diameters (i.e., 1" and 3/4") were used in this work. The results showed that blending CMC with SDBS gives
... Show MoreThe prostaglandins inside inflamed tissues are produced by cyclooxygenase-2 (COX-2), making it an important target for improving anti-inflammatory medications over a long period. Adverse effects have been related to the traditional usage of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammation, mainly centered around gastrointestinal (GI) complications. The current research involves the creation of a virtual library of innovative molecules showing similar drug properties via a structure-based drug design. A library that includes five novel derivatives of Diclofenac was designed. Subsequently, molecular docking through the Glide module and determining the binding free energy implementing the P
... Show MoreMixed ligand of Co and Ni (II) complexes were prepared from [5-(p-nitrophenyl)-4/-phenyl-1,2,4-triazole-3-dithiocarbamato hydrazide](TRZ.DTC) as primary ligand and 2,2'-bipyridyl (bipy) as a co-ligand with metal salts. These complexes were analytically and spectroscopically characterized in solid state by elemental analyses, flame atomic absorption, magnetic susceptibility and molar conductance measurements, as well as by UV–Vis and FTIR spectroscopy. Infrared, ultra violet spectra reveal a bidentate coordination of the two ligands with metal ions 1:1:1 mole ratio. Room temperature magnetic moments and solid reflectance spectra data indicate paramagnetic complexes with five-coordinate square pyramidal geometry for nickel (II) comple
... Show MoreA simple chemistry method approach was used to synthesise new ligand derivate from L-ascorbic acid and its complexes. All of them were water-soluble and are used quite extensively in the medical and pharmaceutical fields. This study synthesised the new ligand derivative from L-ascorbic acid-base using the following steps: A 5,6-O-isopropylidene-L-ascorbic acid was prepared by reacting dry acetone with L-ascorbic acid followed by reacting it with trichloroacetic acid to yield [chloro(carboxylic)methylidene]-5,6-O-isopropylidene-L-ascorbic acid in the second stage. In the third stage, the derivative was reacted with (methyl(6-methyl-2-pyridylmethyl)amine to create a new ligand (ONMILA). This novel ligand was identified using a number
... Show MoreNew derivatives of pyromellitamic diacids and pyromellitdiimides have been prepared by the reaction of one mole of pyromellitic dianhydride with two moles of aromatic amines, these derivatives were characterized by elemental analysis, FT-IR and melting point.