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 increasing requirement and use of dental implant treatments has rendered dental implantology indispensable in dentistry. The aim of this study is to determine the optimum concentration of calcium silicate to be incorporated into a polyetherketoneketone (PEKK) matrix used as an implant material to enhance the bioactivity and mechanical properties of the composite compared with unmodified PEKK. In this study, different weight percentage (wt%) of micro-calcium silicate (m-CS) is incorporated into PEKK with ethanol as a binder. Subsequently, the mixture is dried in a forced convection oven at 120°C and poured into customized molds to fabricate a bioactive composite via compression molding (310°C, 15 MPa, and 20 min holding time
... Show MoreNanocrystalline copper sulphide (Cu2-xS) powders were synthesized by chemical precipitation from their aqueous solutions composed of different molar ratio of copper sulfate dehydrate (CuSO4.5H2O) and thiorea (NH2)2CS as source of Cu+2, S-2 ions respectively, and sodium ethylene diamine tetra acetic acid dehydrate (EDTA) as a complex agent. The compositions, morphological and structural properties of the nanopowders were characterized by energy dispersive spectroscopy (EDS), scanning electron microscope (SEM), and X-ray diffraction (XRD), respectively. The compositional results showed that the copper content was high and the Sulfur content was low for both CuS and Cu2S nanopowders. SEM images shows that all products consist of aggregate o
... Show MoreThis research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea
... Show MoreKE Sharquie, AA Noaimi, MR Al-Karhi, Journal of Cosmetics, Dermatological Sciences and Applications, 2014 - Cited by 2
The new azo dye was prepared from the reaction of the diazonium salt derived from 3-aminophenol with 2- hydroxyquinoline, then it was used to prepare a series of complexes with the chlorides of cobalt, chromium, copper, nickel, platinum, palladium and ammonium molybdate. The ligand was identified by a proton and carbon nuclear magnetic resonance spectroscopy, and the compounds were collected. The prepared materials were subjected to infrared, ultraviolet-visible, and mass spectrometry, as well as thermogravimetric analysis, differential calorimetry, and elemental analysis. Conductivity, magnetic susceptibility, metal content, and chlorine content of the complexes were also measured. The results showed that the ligand behaves in a trigonal b
... Show MoreThis work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,
... 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 More4-Amino-N-(5-methyl-isaxazol-3-yl)-benzenesulfonamide, a new azo (LH) ligand, was synthesized by reacting the diazonium salt of Sulfamethoxazole with coupling compound 3-amino phenol. Spectroscopic techniques (UV-Vis, FTIR, 1H &13C-NMR, and LC-Mass) as well as micro elemental analyses (C.H.N.O) and TGA and SDC were used to identify the azo ligand. Complexes of (Zn(II), Cr(III), Cu(II) and VO(II)) were produced and characterized by atomic absorption, elemental microanalysis, infrared, LC-Mass, TGA, DSC and UV-Vis spectral techniques, as well as conductivity and magnetic quantifications. All the complexes had a 1:2 metal-ligand ratio, and non-electrolytes at all complexes and tetrahedral geometry suggested except Cr-complex, which demonstrate
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