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.
A research include of synthesized five member ring, which has been synthesized by condensation of 2-(1-(4- hydroxyphenyl) ethylidene)hydrazine-1-carbothioamide[I] with α-chloro ethylacetate in sodium acetate (fused) to form ethyl 2-(4-(1-((4-oxo-2-thioxopyrrolidin-3-ylidene)hydrazono) ethyl)phenoxy)acetate [II]. After that reacted [II]with hydrazine hydrate to resulting compound [III]. Compound [III] was refluxed with 4-aminobenzoicacid in excess of phosphorus oxy chloride give compound [IV],the later compound [IV] interact with acetyl acetone or ethylacetoacetate give to pyrazole and pyrazoline derivatives[V],[VI]. While when reacted with different aromatic aldehydes and one ketone consistence Schiff base derivatives [VII]a-e . The FTIR a
... Show MoreThis work illustrates an enhanced visible light photocatalytic degradation of methyl orange dye (M.O.) by employing BiOI / BiOCl composites prepared under room temperature and without any organic precursors. Various experimental parameters have been studied, namely; composition of the composite, irradiation time and cell material. Composition D which implied 75% BiOI and 25% BiOCl has shown the highest bleaching of M.O. dye. This confirms the optimum photo-sensitization phenomenon for this composition in comparison to others. In the optimum photo-sensitized composite the electron of the conduction band reveals better reducing power and the hole of the valence band exhibits more oxidative power than those of pure BiOI electron and hole. Acco
... Show MoreFive N-substituted acrylamides were prepared by reaction of substituted aromatic primary amines with acryloyl chloride in the presence of triethyl amine. The synthesized acrylamides were allowed to introduce copolymerization reaction with three vinylic monomers including acrylonitrile, methyl acrylate and methyl methacrylate respectively to obtain eleven new copolymers having different physical properties which may used in different applications.
Abstract
The target derivative are gentamicin linked with L-Val- L-Ala by an ester linkage. These were synthesized by esterification method, which included the reaction of -OH hydroxyl group on (carbon No.5) of gentamicin with the acid chloride of the corresponding dipeptide, The preparation of new derivative of gentamicin involved protected the primary & secondary amine groups of Gentamicin, by Ethylchloroformate (ECF) to give N-carbomethoxy Gentamicin which was used for further chemical synthesis involving the free hydroxyl groups.
Then prepared dipeptide (L-Val- L-Ala) by conventional solution method in present DCC & HoBt then reacted with thionyl
... Show MoreAntimony selenide substituted with Sb0.4Se0.6 and doped with zinc at three doping ratios (x=0, 0.01 and 0.03) was prepared via the solid state reaction method. The three prepared compositions were reacted thermally at 400 °C for 3 h. The structure of specimens was characterised via X-ray powder diffractometer to obtain the type of crystalline structure and lattice parameters of the prepared specimens, which showed a polycrystalline, orthorhombic structure. Optical characterisation was then achieved via UV-visible spectroscopy to exhibit the transmittance and reflectance spectra and estimate the band gap values of the prepared compositions. The samples showed high abs
... Show MoreQuinolones L1 (ciprofloxacin) are manufactured wide range anti-infection agents with great oral ingestion and magnificent bioavailability. Because of the concoction capacities found on their core (a carboxylic corrosive capacity at the 3-position) and much of the time an essential piperazinyl ring (or anothertN-heterocycle) at the 7-positionh and a carbonylvoxygenc atomi atothel 4-positioni) quinolones bind metal particlesiframing buildings which can go about as bidentate. Bidentateiligands L2=2-phenyl-2-(P-methoxy anilinee) acetonitrilel was set up by the response of Primiryiaminejwithjbenzaldehyde, in nearness of potassiumbcyanidej and acidicimedia . Theimetalledifices were portrayed by the miniaturized scale component examination (C.H
... Show MoreA low speed open circuit wind tunnel has been designed, manufactured and constructed at the Mechanical Engineering Department at Baghdad University - College of Engineering. The work is one of the pioneer projects adapted by the R & D Office at the Iraqi MOHESR. The present paper describes the first part of the work; that is the design calculations, simulation and construction. It will be followed by a second part that describes testing and calibration of the tunnel. The proposed wind tunnel has a test section with cross sectional area of (0.7 x 0.7 m2) and length of (1.5 m). The maximum speed is about (70 m/s) with empty test section. The contraction ratio is (8.16). Three screens are used to minimize flow disturbances in the test section.
... Show MoreThe project has been described the design and construction of a reliable optical testing platform used for evaluate the reflectivity of metal surfaces treated with special paintings required for laser beam attenuation. The platform comprises an Nd-YAG laser system which has been designed and fabricated with specifications to be compatible with their corresponding in laser range finder transmitters used for various applications. The reflectivity of various attenuating paintings, at different detection angles, has been observed. Moreover, the variation of the reflected energy with painting type and metal type to be painted has been studied experimentally. Results illustrated the existence of a definite angle, at which the reflectivity was max
... Show MoreTheoretical study computerized has been carried out in field electron optics , to design electrostatic unipotential lens , the inverse problem is important method in the design of electrostatic lenses by suggesting an axial electrostatic potential distribution using polynomial function. The paraxial –ray equation is solved to obtain the trajectory particles that satisfy the suggested potential function. In this research , design electrostatic unipotential lens three-electrode accelerating and decelerating L=5 mm operated under finite and infinite magnification conditions. The electrode shape of the electrostatic lens was then determined from the solution of the Laplace's equation's. the results showed low values of spherica
... Show MoreAir pollution is one of the important problems facing Iraq. Air pollution is the result of uncontrolled emissions from factories, car exhaust electric generators, and oil refineries and often reaches unacceptable limits by international standards. These pollutants can greatly affect human health and regular population activities. For this reason, there is an urgent need for effective devices to monitor the molecular concentration of air pollutants in cities and urban areas. In this research, an optical system has been built consisting of aHelium-Neonlaser,5mWand at 632.8 nm, a glass cell with a defined size, and a power meter(Gentec-E-model: uno) where a scattering of the laser beam occurs due to air pollution. Two pollutants were examin
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