Synthesis, crystal structure, DNA interaction and cleavage activities of mononuclear and trinuclear copper(II) complexes

Mono- and trinuclear copper(II) complexes with 2-1-(2-dimethylamino-ethylamino)-ethyl]-phenol (HL) have been synthesized and structurally characterized. The mononuclear complex Cu(L)(H2O)(ONO2)] (1) crystallizes in monoclinic space group P2(1) /n with a square pyramidal Cu(II) center coordinated by the tridentate Schiff base (L) and a water ligand in the equatorial plane and an oxygen atom from nitrate in the axial position. The trinuclear complex (CuL)(3)(mu(3)-OH)](ClO4)(2)center dot H2O (2) crystallizes in hexagonal space group P6(3); all three copper atoms are five-coordinate with square pyramidal geometries. The interactions of these complexes with calf-thymus DNA have been investigated using absorption spectrophotometry. The mononuclear complex binds more strongly than the trinuclear complex. The DNA cleavage activity of these complexes has been studied on double-stranded pBR 322 plasmid DNA by gel electrophoresis experiments in the absence and in the presence of added oxidant (H2O2). The trinuclear complex cleaves DNA more efficiently than the mononuclear complex in the presence of H2O2.

Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 mu g/mL) and Penicillium chrysogenum (38 mm, MIC 12.5 mu g/mL). The amino linked pyrimidinyl bis benzothiazole 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 mu M. (C) 2014 Elsevier Masson SAS. All rights reserved.

Syntheses and structural investigation of some alkali metal ion-mediated (LVO2-)-O-V (L2- = tridentate ONO ligands) species: DNA binding, photoinduced DNA cleavage and cytotoxic activities

Eight alkali metal ion-mediated dioxidovanadium(V), {(VO2L1-6)-O-V} A(H2O)n]proportional to, complexes for A = Li+, Na+, K+ and Cs+, containing tridentate aroylhydrazonate ligands coordinating via ONO donor atoms, are described. All the synthesised ligands and the metal complexes were successfully characterised by elemental analysis, IR, UV-Vis and NMR spectroscopy. X-ray crystallographic investigation of 3, 5-7 shows the presence of distorted NO4 coordination geometries for LVO2- in each case, and varying mu-oxido and/ or mu-aqua bridging with interesting variations correlated with the size of the alkali metal ions: with small Li+, no bridging-O is found but four ion aggregates are found with Na+, chains for K+ and finally, layers for Cs+. Two (5) or three-dimensional (3, 6 and 7) architectures are consolidated by hydrogen bonding. The dioxidovanadium(V) complexes were found to exhibit DNA binding activity due to their interaction with CT-DNA by the groove binding mode, with binding constants ranging from 10(3) to 10(4) M-1. Complexes 1-8 were also tested for DNA nuclease activity against pUC19 plasmid DNA which showed that 6 and 7 had the best DNA binding and photonuclease activity; these results support their good protein binding and cleavage activity with binding constants ranging from 104 to 105 M-1. Finally, the in vitro antiproliferative activity of all complexes was assayed against the HeLa cell line. Some of the complexes (2, 5, 6 and 7) show considerable activity compared to commonly used chemotherapeutic drugs. The variation in cytotoxicity of the complexes is influenced by the various functional groups attached to the aroylhydrazone derivative.

Synthesis and Antioxidant Activities of Novel Chiral Ebselen Analogues

Novel chiral analogues of the antioxidant, anti-inflammatory organoselenium drug ebselen were synthesized. The reaction proceeded readily from 2-(chloroseleno)benzoyl chloride with chiral amino compounds. The chiral substituent on the nitrogen atom did not provide a substantial increase in activities and the newly synthesized compounds showed similar activities to ebselen.

Phase transformation of ZrO2:Tb3+ nanophosphor: Color tunable photoluminescence and photocatalytic activities

The current study involves synthesis of a series of Tb3+ doped ZrO2 nanophosphors by solution combustion method using oxalyl dihydrazide as fuel. The as-formed ZrO2:Tb3+ nanophosphors having different concentrations of Tb3+ (1-11 mol%) were characterized by powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and UV-Visible spectroscopic techniques and the materials were subjected to photoluminescence and photocatalytic dye decolorization studies. The PXRD analysis indicates the formation of tetragonal symmetry up to 5 mol% concentration of Tb3+. Further increase in Tb3+ concentration has lead to cubic phase formation and the same was confirmed by Rietveld refinement analysis. SEM images revealed that material was highly porous in nature comprising of large voids and cracks with irregular morphology. TEM and SAED images clearly confirm the formation of high quality tetragonal nanocrystals. The emissive properties of nanophosphors were found to be dependent on Tb3+ dopant concentration. The green emission of the material was turned to white emission with the increase of Tb3+ ion concentration. The photocatalytic activities of these nanophosphors were probed for the decolorization of Congo red under UV and Sunlight irradiation. All the photocatalysts showed enhanced activity under UV light compared to Sunlight. The photocatalyst with 7 mol% Tb3+ showed enhanced activity attributed to effective separation of charge carriers due to phase transformation from tetragonal to cubic. The influence of crystallite size and PL on charge carrier trapping-recombination dynamics was investigated. The study successfully demonstrates synthesis of tetragonal and cubic ZrO2:Tb3+ green nanophosphors with superior photoluminescence and photocatalytic activities. (C) 2014 Elsevier B.V. All rights reserved.

Synthesis, antioxidant, and cytotoxic activities of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl Acetamides

A new class of bis(oxazolyl/thiazolyl/imidazolyl)amidomethanesulfonyl acetamides was prepared from the respective (oxazolyl/thiazolyl/imidazolyl)carbamoyl-methylthio acetic acid and studied their antioxidant activity and cytotoxic activitity against A549 lung adenocarcinoma cells. The methyl-substituted sulfonyl bisoxazoles exhibited excellent radical scavenging activity. On the other hand, the chloro-substituted sulfonyl bisthiazoles (IC50 = 49 A mu M) and sulfonyl bisimidazoles (IC50 = 24 A mu M) showed noticeable cytotoxic activity on A549 cells.

Radical Scavenging and Antimicrobial Activities of Methanol Extracts of Two Kinds of Formicary

对两种不同的蚂蚁窝进行甲醇提取,并对提取物进行了急性毒性、抗自由基,酚含量、还原能力和抗菌活性的检测。二苯基三硝基肼(1,1-diphenyl-2-picrylhydrazyl,DPPH)自由基的清除能力的检测表明:两种蚂蚁窝甲醇提取物都具有显著的自由基清除能力,并呈现出剂量依赖性,而且,在高浓度时(5~10mg·mL-1),它们的自由基清除能力甚至显著地高于二丁基羟基甲苯(butylated hydroxyl toluene,BHT)。酚的含量和还原能力分别用福林酚试剂和铁氰化钾还原反应来测定,统计分析显示两种蚂蚁窝的抗氧化能力和其酚含量、还原能力都存在着正相关。两种蚂蚁窝甲醇提取物都具有抗革兰氏阴性菌和革兰氏阳性菌的活性,但它们却对真菌没有作用。

Indole and carbazole alkaloids from Glycosmis montana with weak anti-HIV and cytotoxic activities

A diprenylated indole, (E)-3-(3-hydroxymethyl-2-butenyl)-7-(3-methyl-2-butenyl)-1H-indole (1), and six known carbazole alkaloids were isolated from the twigs and leaves of Glycosmis montana Pierre (Rutaceae). Their structures were determined on the basis of analysis of spectral evidence including 1D and 2D NMR and MS. The alkaloids (1-3) exhibited weak to moderate take in vitro inhibitory activity against HIV replication in C8166 cells, and they (as well as carbalexine A and B) had cytotoxic activity against the human leukaemia cell line CCRF-CEM. (c) 2005 Elsevier Ltd. All rights reserved.

Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities

Twelve novel zidovudine derivatives were prepared by modifying 5 '-hydroxyl group of sugar moiety (1-8) and 5-methyl group of thymidine nucleus (9-12) and characterized spectrally. The compounds were evaluated for anti-HIV-1, antitubercular and antibacter