5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds. ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed enhanced cytotoxic effects for [IV] over 5-FU.
The flexibility of interaction between the movement of macroeconomic variables that affect and are affected by the balance of payments, especially the movement of the current account, implies a perception of the maturity of economic development and what the theory assumes from the launch of a wide range of economic movement that varies in the degree of its influence according to the level of economic development and the vitality of the internal/external overlap relations through the assumed response to the movement of the macroeconomic variables. On this basis, it is possible to estimate the soundness and rationality of the economic decision taken that takes into account the required reciprocal repercussions between the current a
... Show MoreAzo ligand 4-((2-hydroxy-3,5-dimethylphenyl)diazenyl) benzoic acid was synthesized from 4-aminobenzoic acid and 2,4- dimethylphenol. Azo dye compounds have been characterized by different techniques (1H-NMR, UV-Vis and FT-IR). Metal chelates of (ZnII, CdII and HgII) have been synthesized with azo ligand (L). Produced compounds have been identified by using spectral studies, elemental analysis(C.H.N.) and conductivity. Produced metal chelates were studied using mole ratio as well sequences contrast types. Rate of concentration(1×10-4-3×10-4 Mole/L) sequence Beer's law. Compound solutions have been noticed height molar absorptivity. The addendum of ligand and compounds has applied as disperse dyes on cotton fabrics for antibacterial activit
... Show MoreNew complexes of the some trivalent transition metal ions of the uracil such as [M(Ura)3Cl3] and mixed ligand metal complexes with uracil and oxalic acid [M(Ura)2(OA)(OH2)Cl].H2O type, where (Ura)=Uracil, (OA= Oxalic acid dihydrate, (M= Cr+3 and Fe+3) were synthesized and characterized by the elemental analysis, FT.IR, electronic spectra, mass spectra and magnetic susceptibility as well as the conductivity measurements. Six–coordinated metal complexes were suggested for the isolated complexes of Cr+3 and Fe+3 with molecular formulas dependent on the nature of uracil and oxalic acid present. The proposed molecular structure for all complexes with their ions is octahedral geometries. The antibacterial efficiency was tested of metal salts, l
... Show More4-amino-3-(4-(((4-hydroxy-3,5dimethoxybenzyl)oxy)methyl)phenyl)-1,2,4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3,5-dimethoxybenzyl)oxy)methyl)benzoyl)hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1,2,4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays were used to scree
... Show MoreThe preparation of some new coordination compounds for nikel (II), manganese (II), copper (II), cobalt (II)and mercury (II), with ligand obtained from Benzoinand2-amino pyridine.The ligand[6-(2-hydroxy-1,2-diphenylethylideneamino)pyridin-3-ylium)](L) was made from reactin ethanol with metal salts in (1:1)(metal : ligand)ratio.[MLCl] was the inclusive formula of the complexes where M= Mn(II),Co(II),Ni(II),Cu(II) and Hg(II). Metal analysis by electronic spectra, atomic absorption ,infrared spectra, 1H&13C-NMR(only ligand)spectral studies, magnetic moment and molar conductance measurements used to describe the compounds.The determinations indicated that the ligand coordinates with the metal (II) ion in neutral tridentate manner th
... Show MoreAn oral bi layer sustained release (SR) strips of Sodium Montelukast SMLT , which is selective leukotriene antagonist , used for patients suffered from mid-night asthma , were prepared successfully ,using different polymers, like guar gum , carrageenan , and xanthan gum , by solvent casting method .
The results obtained by this study revealed ,that best fast dissolving film of SMLT was loaded in carrageenan polymer 57% w\w (30mg.) , with acceptable physical properties, like film thickness , elastic endurance and surface pH .
Besides to that , the disintegration t
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This research included the preparation and characterization of new demulsifies from natural and synthetic polymers of chitosan and polyvinyl alcohol that are environmentally friendly and at the same time have high efficacy comparable to emulsifiers. imported foreign. The prepared compounds were examined using infrared spectroscopy and nuclear magnetic resonance spectroscopy, and all the spectral signals of the polymers were in good agreement with the chemical composition of the polymers. And the melting and decomposition that occur on polymers at high temperatures. The effect of the length and type of side chain in the compositions of polymers on the process of water separation of oil emulsions w
... Show MoreThis paper deals with the preparation of new monomers and polymers which including heterocyclic unit. The diacid chlorides compounds [1-3] were prepared from the reaction of glutaric acid, adipic acid, terephthalic acid with thionyl chloride. Succinic acid reacted with ethanol to produce compound [4]. Compound [4] reacted with hydrazine hydrate to obtain succinic hydrazide [5].Compound [5] reaction with CS2 and KOH in absolute ethanol to produce compound [6].The polymers [7-12] have been created by reacting diacid chlorides compounds [1-3] with compound[5] or [6] in dry pyridine with some drops of DMF. The topology of produced compounds has characterized through their spectral and analytical data as in FT-IR spectra, Thermal analysis [DSC,
... Show MoreThe present paper describes the synthesis and structural studies of new transition metal complexes of cobalt(II), nickel(II), copper(II) and cadmium(II) with two bi dentate ligands derived from quinoxaline-2,3-dione. The two ligands were fully identified by elemental analyses, FT-IR, NMR and UV-Visible spectra. The metal complexes of Co(II), Ni(II), Cu(II) and Cd(II) were isolated in the solid state after reactions of their metal chlorides with the ligands in 2:1 mole ratio. The isolated solid metal complexes were characterized with the help of elemental analyses, NMR, FT-IR and UV-Visible spectra. As well as the thermal stability of the coordinated quinoxaline polymers were tested by TG-DSC analysis and it is found th
... 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
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