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.
Three Schiff bases from Benzaldehyde and Salicylaldehyde have been synthesized (A, 1and 2) and two of them (1and 2) have been tested for anti-inflammatory activity. The p-aminobenzene sulfonamide has been synthesized from acetanilide through the addition of excess chlorosulfonic acid then concentrated ammonia solution; Schiff base of this derivative (2) exhibited good level of activity against egg-white induced edema in rat hind paw, while the other tested derivative exhibited no activity.
Key words: Schiff bases, sulfonamide derivatives, salicylaldehyde
A new class of biologically active nanocomposites and modified polymers based on poly (vinyl alcohol) (PVA) with some organic compounds [II, IV, V and VI] were synthesized using silver nanoparticles (Ag-NPs). All compounds were synthesized using nucleophilic substitution interactions and characterized by FTIR, DSC and TGA. The biological activity of the modified polymers was evaluated against: gram (+) (staphylococcus aureus) and gram (-): (Es cherichia coli bacteria). Antimicrobial films are developed based on modified poly (vinyl alcohol) MPVA and Ag-NPs nanoparticles. The nanocomposites and modified polymers showed better antibacterial activities against Escherichia coli (Gram negative) than against Staphyloc
... Show MoreMixed ligand metal complexes of CrIII, FeIII,II, NiII and CuII have been synthesized using 5-chlorosalicylic acid (5-CSA) as a primary ligand and L-Valine (L-Val) as secondary ligand. The metal complexes have been characterized by elemental analysis, electrical conductance, magnetic susceptibility measurements and spectral studies. The electrical conductance studies of the complexes indicate their electrolytic nature. Magnetic susceptibility measurements revealed paramagnetic nature of the all complexes. Bonding of the metal ion through –OHand –COOgroups of bidentate to the 5-chlorosalicylic acid and through –NH2 and –COOgroups of bidentate to the L-valine by FT-IR studies . The agar diffusion method has been used to study the antib
... Show MoreHybrid architecture of ZnO nanorods/graphene oxide ZnO-NRs@GO synthesized by electrostatic self-assembly methods. The morphological, optical and luminescence characteristics of ZnO-NRs@GO and ZnO-NRs thin films have been described by FESEM, TEM, HRTEM, and AFM, which refers to graphene oxide have been coated ZnO-NRs with five layers. Here we synthesis ZnO-NRs@GO by simple, cheap and environmentally friendly method, which made it favorable for huge -scale preparation in many applications such as photocatalyst. ZnO-NRs@GO was applied as a photocatalyst Rodamin 6 G (R6G) dye from water using 532 nm diode laser-induced photocatalytic process. Overall degradation of R6G/ ZnO-NRs@GO was achieved after 90 minutes of laser irradiation while it ne
... Show MoreThis study aimed to assess the possible association of oxytocin (OXT) gene with reproductive traits in two groups of Awassi ewes that differ in their reproductive potentials. Sheep were genotyped using PCR—single-stranded conformation polymorphism approach. Three genotypes were detected in exon 2, CC, CA, and AA, and a novel SNP was identified with a missense effect on oxytocin (c.188C > A → p.Arg55Leu). A significant (p < 0.01) association of p.Arg55Leu with the twinning rate was found as ewes with AA and CA genotypes exhibited, respectively a lower twinning ratio than those with the wild-type CC genotype. The deleterious impact of p.Arg55Leu was demonstrated by all in silico tools that were utilized to assess the effect of this varian
... Show MoreThis research paper studies the use of an environmentally and not expensive method to degrade Orange G dye (OG) from the aqueous solution, where the extract of ficus leaves has been used to fabricate the green bimetallic iron/copper nanoparticles (G-Fe/Cu-NPs). The fabricated G‑Fe/Cu-NPs were characterized utilizing scanning electron microscopy, BET, atomic force microscopy, energy dispersive spectroscopy, Fourier-transform infrared spectroscopy and zeta potential. The rounded and shaped as like spherical nanoparticles were found for G-Fe/Cu‑NPs with the size ranged 32-59 nm and the surface area was 4.452 m2/g. Then the resultant nanoparticles were utilized as a Fenton-like oxidation catalyst. The degradation efficiency of
... Show MoreAbstract New derivatives of 1,2,4- triazole , 1,2,4-triazole -3-one and 1,2,4-triazole-3-thione were obtained through this research. Acid hydrazide derivative was present from reaction of poly acryloyl chloride with hydrazine hydrate in presence of DMF as a solvent then reacted with benzonitrile and its derivatives to give 1,2,4-triazole derivatives. After that reaction of poly acryloyl chloride with semicarbazide and semithiocarbazide to form semicarbazone and semithiocarbazone derivatives respectively. Finally, closing of semicarbazone and semithiocarbazone derivatives with 2% NaOH gave 1,2,4-triazole -3-one and 1,2,4-triazole-4-thione derivatives respectively. These new synthesized products have been characterized by infrared, 1 H-n
... Show MoreABSTRACT. The reaction between benzil and hexamethylenediamine formed a new ligand [L], [(1Z,3Z)-2,3-diphenyl-5,6,7,8,9,10-hexahydro-1,4-diazecine], of the type [N2], was synthesized by the condensation reaction through Schiff base reaction between benzil and hexamethylenediamine. The new Schiff base ligand reacts with Mnп, Niп and Coп metal ions to give the complexes with the general formula: [M(L)Cl2]. The elemental investigations have been used to analyze the ligand and its complexes by CHN, FT-IR, UV-Vis, TLC, mass spectrum, melting point with the study of biological activity to the formed compounds. From the data obtained, the proposed molecular structure adopts square planar structure about the metal ions. The study reveals
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