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.
Design and construction of video extractor circuit require an understanding of several parameters, which include: Selector circuit, extracting circuit which contains sampling signal and multiplexing. At each radar pulse, the video signal is fed to one of the selector. The fast filter has a pass –band from 190 Hz to 1800 Hz. These frequencies correspond to targets having radial velocities laying between and 10 Kph and 200 Kph.Slow filter: 60 Hz to 230 Hz for radial velocities laying between 3.5 and 13 Kph.The video- extractor is organized in four PCB CG (A-B-C-D) each one having 16 selector. The sampling signal (ADS) (1-2-3-4) control the 4-line-to-16-line decoders. 8 multiplexers of 8 inputs each, are required for the multiplexing of the
... Show MoreReduction represents a form of artistic abstraction to express things with formal symbols that suggest the content of the idea, as the beauty of the design artwork cannot be unique in the form only, but in revealing its meaning as well. He resorts to shorthand to express the content of his idea related to design necessities and needs to achieve a specific function whose role is crystallized through the form that follows the function. The importance of the research was also represented in: Benefiting workers and scholars in the field of design with regard to shorthand and implicit in graphic design. The aim of the research: to identify the relationship between implicit meaning and reduced forms in graphic design. And the aesthetic of fo
... Show MoreIn this work the design and construction of optical pumping system was presented. The parameters of the pumping source to obtain discharge current density sufficient to shift the flash lamp spectrum towards uv portion of spectrum were measured.The current density was supplied to the flash lamp must be greater than 4000Amp./cm2 to obtain the spectral range wavelength lies between 0.2 and 0.35?m. The current density was obtained by a capacitor 50?F, at 7KV discharge voltage. The applied electrical energy to the flash lamp was more than 1200 J, and the current density was around 5000 Amp./cm2.The electrical parameters of the flash lamp were calculated. The impedance parameters(K0) from the voltage and the peak current pulse was measured in ran
... Show MoreIn this work the design and construction of a flash photolysis pulsed HCl laser was presented. The parameters of the pumping source and discharge current density was obtained, which sufficient to shift the flash lamp spectrum towards uv portion of spectrum. The maximum pulse laser energy parameters was measured. Total pressure and ratio of active gases to optimized the output pulse energy were measured , where at 125 mbar of total pressure and 1:7:14 Cl2:H2: He ratio, the laser energy was measured to be 200 mJ at pumping four flash lamps energy in the order of 6400J .The resonator consists of copper a near hemispherical mirror with the radius of curvature 3m coated by gold and reflectivity 98%,the output coupler sapphire mirror of
... Show MoreNew series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hy
... Show MoreNew series of 4, 4'-((2-(Aryl)-1H-benzo [d] imidazole-1, 3 (2H)-diyl) bis (methylene)) Diphenol (3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr
... Show MoreThe 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
... Show MoreThe 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.
... Show MoreThe 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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