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Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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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.

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Publication Date
Sat Oct 01 2022
Journal Name
Inorganic Chemistry Communications
Synthesis, characterization, and bioactivity of several metal complexes of (4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide)
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4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide was synthesized by reacting the diazonium salt of sulfamethoxazole with 3-amino phenol. Complexes of Ni(II), Pd(II), Au(III), and Pt(IV) were produced and characterized by atomic absorption, elemental microanalysis, infrared spectroscopy, liquid chromatography–mass spectroscopy, thermogravimetric analysis, different scanning calorimetry, and ultraviolet–visible spectroscopy. Furthermore, the conductivity and magnetic properties were quantified. According to the analytical studies, all complexes were found to possess a 1:2 metal–ligand ratio and were non-electrolytes, except the Au(III) complex electrolyte, which had a 1:1 metal:ligand ratio. The biological activities of some of the

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Publication Date
Sat Oct 01 2022
Journal Name
Inorganic Chemistry Communications
Synthesis, characterization, and bioactivity of several metal complexes of (4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide)
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Publication Date
Sun Dec 30 2018
Journal Name
Journal Of Pure And Applied Microbiology
Mixture Design of Experiments for the Optimization of Carbon Source for Promoting Undecylprodigiosin and Actinorhodin Production
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Publication Date
Wed Oct 09 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis, characterization, spectral of azo dyes ligands complexes with Rh(III) and La(III) and studies their industrial and bacterial application
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1-[4-(2-Hydroxy-4, 6-dimethyl-phenylazo)-phenol]-ethanone (HL1) and 2-(4-methoxy-phenylazo)-3, 5- dimethyl-phenol (HL2) were produced by combination the diazonium salts of amines with 3, 5- dimethylphenol. The geometry of azo compounds was resolved on the basis of (C.H.N) analyses, 1H and 13CNMR, FT-IR and UV-Vis spectroscopic mechanisms. Complexes of La (III) and Rh (III) have been performed and depicted. The formation of complexes has been identified by using elemental analysis, FTIR and UV-Vis spectroscopic process as well, conductivity molar quantifications. Nature of complexes produced have been studied obeyed mole ratio and continuous alteration ways, Beer's law followed through a concentration scope (1×10-4 - 3×10-4 M). High molar

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Publication Date
Wed Jun 16 2021
Journal Name
Biochemical And Cellular Archives
Synthesis, characterization and pharmaceutical studies of schiff base from 2-pyrrolidinone derivative and imidazole-2-carboxaldehyde and corresponding complexes with Metal (||)
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Synthesis, characterization and pharmaceutical studies of schiff base from 2-pyrrolidinone derivative and imidazole-2-carboxaldehyde and corresponding complexes with Metal (||)

Publication Date
Sat Apr 29 2023
Journal Name
Research Journal Of Pharmacy And Technology
Effect of Omega 7 on Some Parameters Related to WBCs and RBCs in Methotrexate-induce Blood Toxicity in Mice
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Background: Although methotrexate (MTX) is a frequently used chemotherapy drug, its effectiveness is sometimes hampered by the drug's toxic consequences. Omega 7 is a monounsaturated fatty acid, with different anti-inflammatory, anti-diabetic anti-obesity applications, and its possible protective effects against MTX-induced blood toxicity were investigated in this study. Objective: Evaluation of possible protective effects of omega7 against MTX-induced blood toxicity. Methods: 30 mice were divided into five groups, the First group take liquid paraffin orallyfor 7 days for served as negative control and the second group take methotrexate (20mg/kg) intraperitoneallyto serve as a positive control,the third group takes omega 7 (100mg/kg

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Publication Date
Tue Jan 01 2019
Journal Name
Energy Procedia
Fabrication and characterization of n-InSb Heterojunction for optoelectronic device
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The operating characteristics of optoelectronic devices depend critically on the properties physical of the constituent materials, interesting compound has been focused on this research formed from group III and V of the periodic table. Thin film n-InSb heterjuntion were successfully fabricated on p-Si substrates by thermal evaporation technique at different annealing temperature (as prepared, 400,500,600) °C. The effect of annealing temperature on the structural, surface morphology, optical and optoelectronic properties of InSb films were investigated and studied. The crystal structure of the film was characterized by X-ray diffraction and techniques. AFM techniques inspect the surface morphology of InSb films, the study presented the val

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Publication Date
Sat Jan 05 2019
Journal Name
Iraqi Journal Of Physics
Fabrication and characterization of porous silicon for humidity sensor application
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Porous Silicon (PS) layer has been prepared from p-type silicon by electrochemical etching method. The morphology properties of PS samples that prepared with different current density has been study using atom force measurement (AFM) and it show that the Layer of pore has sponge like stricture and the average pore diameter of PS layer increase with etching current density increase .The x-ray diffraction (XRD) pattern indicated the nanocrystaline of the sample. Reflectivity of the sample surface is decrease when etching current density increases because of porosity increase on surface of sample. The photolumenses (PL) intensity increase with increase etching current density. The PL is affected by relative humidity (RH) level so we can use

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer
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Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.

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Publication Date
Tue Jan 01 2019
Journal Name
Energy Procedia
Fabrication and characterization of n- InSb Heterojunction for optoelectronic device
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