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.
This work involves synthesis and characterization of some new 1, 3, 4-thiadiazole or pyrazoline derivatives heterocyclic containing indole ring. The new 2-amino-1, 3, 4-thiadiazole derivatives [IV] and [V] a, b were synthesized by cyclization reaction of 2-methyl-1H-indole-carbothiosemicarbazide [III] in H2SO4 acid or by reaction of indole-3-acetic acid or indole-3-butanoic acid with thiosemicarbazide in the presence of phosphorous oxychloride, respectively. Amide derivatives [VI]-[VIII] were synthesized by the reaction equimolar of 2-amino-1, 3, 4-thiadiazoles and (acetyl chloride, benzoyl chloride, anisoyl chloride and heptanoyl chloride) in DMF and pyridine as accepter. The new pyrazolone derivatives [XI] a, b were synthesized from heati
... Show MoreHard-grade asphalt binders like AC20-30 typically exhibit excessive stiffness, reduced penetration, and compromised workability, necessitating modification before use in paving applications. This study evaluates the efficacy of regular polyalphaolefin (PAO), a synthetic olefin-based lubricant, as a performance-enhancing modifying agent for such binders. AC20-30 was blended with PAO at dosages ranging from 2 wt.% to 10 wt.%, and the modified binders were characterized via penetration, ductility, softening point, and rotational viscosity measurements, alongside advanced rheological and chemical-morphological analyses. Incorporating PAO in AC20-30 asphalt progressively reduced the binder stiffness and enhanced its flexibility, with all modifie
... Show MoreSchiff base N,N'-Bis-(4-dimethylamino-benzylidene)-benzene-1,4-diamine has been synthesized from 4-dimethylaminobenzenaldehyde and benzene-1,4-diamine. The structure of Schiff base was obtained by (C.H.N.) microanalysis, Mass, 1HNMR, FT-IR and UV-Vis spectral methods and thermal analysis. Metal mixed ligand complexes of some metal(II) salts with Schiff base ligand and anthranilic acid were prepared in the molar ratio (1:2:2), (Metal):(SBL)2:(Anthra)2, (SBL)= Schiff base ligand, (Anthra) =anthranilic acid and Metal= Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II). The thermal behaviour (TGA) of the complexes was studied. The prepared complexes identified by using mass, thermal analysis, FT.IR and UV-Vis spectrum methods, on otherwise flame
... Show MoreTwo compounds,[2-amino-4-(4-nitro phenyl) 1,3-thiazole],(4) and [2-amino-4-(4-bromo phenyl) 1,3-thiazole],(5), were synthesized by refluxing thiourea (1) with each of para-ntiro and para-bomophanacyl bromides(2) and (3) respectively, in absolute methanol. Then, by reaction of [5] with 3,5-dinitrobenzoyl chloride in dimethylformamide (DMF) yielded (6) .On the other hand, reaction of (4) with chloroacetyl chloride in dry benzene afforded (7), which is upon treatment with thiourea in absolute methanol, af
... Show MoreIt is found that hypersensitive teeth have a larger number and wider patent tubules than those of non-sensitive teeth. Objective: The aim of this study is to compare between the effects of diode laser at different power densities, with and without sodium fluoride on the sealing of exposed dentinal tubules and dentin permeability. Materials and methods: 118 teeth were used. Samples were divided into three major groups. The first consisted of 100 teeth used for permeability test. The second consisted of 16 teeth for measuring external surface temperature elevation while irradiation. The third, in turn, consisted of one pair of teeth observed under SEM for dentine surface morphology analysis. Results: For dentin permeability measurement, th
... Show MoreThe study involved the synthesis of new complexes with tetradentate ligand (LH). The general formula of complexes was [M(LH)(H2O)2] with M of Ni2+, Co2+, Cu2+, and Zn+. The ligand was synthesized by treating the 2-hydroxybenzohydrazide with salicylaldehyde. The structural characteristics of ligands and complexes were analyzed using various techniques, including elemental analyses, magnetic susceptibility, molar conductivity, infrared, ultraviolet absorption, mass, and NMR spectroscopy studies. The physical measurements indicated that the prepared complexes are non-electrolyte and showed that the ligand is tetradentate when coordinated with metal ions through the nitrogen of azomethine (–C=N–), two oxygen atoms of O–H phenolic,
... Show MoreAbstract
A series of new 4(3H)-quinazolinone derivatives (S1-S4) were synthesized and characterized by FTIR,1HNMR and 13CNMR .Their cytotoxic activity against a set of human cancer cell lines MCF-7 (breast) and A549 (lung) was evaluated using MTT assay. To detect their selectivity toward cancer cells, the compounds were also tested against epithelial cells derived from normal human fibroblast (NHF). Methotrexate (MTX) was used as a reference for comparison . All the tested compounds exhibited toxicity against the normal cells lower than cancer cells. All the tested compounds displayed higher cytotoxicity against lung cancer cell line (A549) than MTX with the most
... Show MoreThe aim of the work is the synthesis and characterization of the tridentate Schiff base (HL) containing (N and O) as donor atoms type (ONO). The ligand is: (HL) phenyl 2-(2-hydroxybenzylidenamino)benzoate This ligand was prepared by the reaction of (phenyl 2-aminobenzoate) with salicylaldehyde under reflux in ethanol and few drops of glacial acetic acid which gave the ligand (HL). The prepared ligand was characterized by (FT IR,UV–Vis) spectroscopy, Elemental analysis of carbon, hydrogen and nitrogen (C.H.N.) and melting point. The ligand was reacted with some metal ions under reflux in ethanol with (1 metal :2 ligand )mole ratio which gave complexes of the general formula: Pr III , Cr and III La III [M(L)2]Cl , M = Products were found to
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