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.
5-((2,4-dibromo-6-((cyclohexyl(methyl)amino)methyl)phenyl)diazenyl)quinolin-8-ol azo ligand (L) has been synthesized through the reaction of diazonium salt for 2,4-dibromo-6-((cyclohexyl(methyl)amino)methyl)aniline with 8-hydroxyquinoline. The azo ligand (L) was characterized utilizing spectroscopic techniques, including FTIR, UV-Vis, 1H and 13C NMR, as well as mass spectrometry and micro-elemental analysis (C.H.N). Metal complexes containing Co(II), Ni(II), Cu(II), and Zn(II) were synthesized and analyzed through mass spectrometry, flame atomic absorption, elemental analysis (C.H.N), infrared and UV-Vis spectroscopy, along with measurements of conductivity and magnetic properties. The experimental findings suggested that all met
... Show MoreBackground: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreThe topic of context is one of the important topics, which was mentioned as a concept in several fields and different fields, and there were many points of view that defined that concept.
He specified the title of the research (design contexts in the design of the interior space), as the research sought to identify the concept of context in the interior design of the spaces of sewing workshops. The research was divided into four chapters:
The first chapter, which consists of the methodological framework, the problem of research and the need for it, the importance of research, the goal and limits of research for sewing workshops for vocational schools from (2020-2021).
The second chapter: consists of previous studies and the theo
Abstract
The goal of current research to describe and diagnose the level of attention of doctors to design and regulatory dimensions, (strategic vision, organizational structure, organizational processes, business systems, personnel), and the performance of hospitals and dimensions, in six hospitals in medicine and selected a sample for research, as well as identify organizational design effect in the performance of hospitals and dimensions (efficiency, the development of human resources, patient satisfaction, achieve financial results, quality of health care).
Research has focused in part theoretical on key variables to look organizational des
... Show MoreThe work includes synthesis of 1,2,3-triazoles via click conditions and using the microwave irradiation starting from two synthesized azides: 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl azide (5) and perfluorobutylethyl azide (10) and different terminal alkynes. It also includes microwave enhanced synthesis of tetrazoles via the reaction of two synthesized azides i.e., perfluorobutylethyl azide (10) and 1,5-diazidopentane (13) with benzoyl cyanide. Most of the prepared compounds have been characterized by: TLC, FT-IR, 1H NMR, 13C NMR, LC-MS and microelemental analysis
In this paper had been studied the characterization of the nanocatalyst (NiO) Mesh electrodes. For fuel cell. The catalyst is prepared and also the electrodes The structural were studied through the analysis of X-ray diffraction of the prepared nanocatalyst for determining the yielding phase and atomic force microscope to identify the roughness of prepared catalyst surface, Use has been nanocatalyst led to optimization of cell voltage, current densities & power for a fuel cell.
The biological activities of some ternary nickel complexes with a Schiff base obtained from 4-dimethylaminobenzaldehyde and 2-aminophenol have been reported. The Schiff base ( HL1) acts as a primary ligand whereas, anthranilic acid ( HL2), 2-nitroaniline ( HL3), alanine ( HL4) and histidine ( HL5) act as secondary ligand or co-ligand. The anticancer activity of these compounds was studied against human colon carcinoma (HCT-116), human hepatocellular liver carcinoma (HEPG-2) and human breast carcinoma (MCF-7) cell lines. As per the results, the compounds were active against the cell lines. The antioxidant activity of the same compounds was evaluated using DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical scavenging and compared with ascorbic aci
... Show More2,2'-(1-(3,4-bis(carboxydichloromethoxy)-5-oxo-2,5-dihydrofuran-2-yl)ethane-1,2-diyl)bis(oxy)bis(2,2-dichloroacetic acid) a derivative of L-ascorbic acid was prepared by reaction of L-ascorbic acid with trichloroacetic acid (1:4) ratio, in the presence of potassium hydroxide. A series of new metal complexes of this ligand were prepared by a reaction with the chlorides of Cd(II), Co(II), Ni(II), Cu(II) and Zn(II). The new ligand and its complexes were identified by C.H.N., IR, UV-visible spectra, Thermogravimetric analysis (TGA), as well as 1H, 13C-NMR and Mass spectra for ligand L. The complexes were also identified by molar conductance, atomic absorption, magnetic susceptibility and X-ray diffraction for Cu (II) complex. FT-IR spectra
... Show MoreHighly-fluorescent Carbon Quantum Dots (CQDs) are synthesized in simple step by hydrothermal carbonization method of natural precursor such as orange juice as a carbon source. Hydrothermal method for synthesized CQDs requires simple and inexpensive equipment and raw materials, thus this method are now common synthesis method. The prepared CQDs have ultrafine size up to few nanometers and several features such as high solubility in water, low toxicity, high biocompatibility, photo-bleaching resistant, Chemical inertness and ease of functionalization which qualifies it for use in many applications such as bio-imaging, photo-labeling and photo-catalysis.
This research demonstrates the
... Show MoreA tetradentate (N2O2) Schiff base (H2Ldfm) was successfully synthesized via condensation of curcumin / diferuloylmethane (dfm) and L-leucine amino acid (HL). There were three different methods that used for synthesizing H2Ldfm; (refluxing, grading, and fusion). Ten different metal complexes were also successfully synthesized by combination of the Schiff base (H2Ldfm) and 1,10-phenanthroline (phen) ligand to form a hexadentate (N4O2) mixed ligands (Ldfm , phen) with ten different metal salts (M) where{ M= Al(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Ag(I), Cd(II), Hg(II), and Pb(II)}. The molar ratio of reactants was (1:1:1) (M: H2Ldfm : phen). The new Schiff base and its new complexes were characterized by different physicochemical tec
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