New, Substituted Derivatives of Dicarboximides and their Cytotoxic Properties.

A large group of aminoalkyl and aminoalkanol derivatives of selected dicarboximides were synthesized and characterized by 1HNMR, 13CNMR and ESI MS spectra analysis. The thirty nine new compounds were tested for their cytotoxic properties in human chronic (K562), acute leukemia (HL-60), and cervical cancer cells (HeLa) as well as in normal endothelial cells (HUVEC). The most promising compounds are 4-[2-(dimethylamino)ethyl]-, (diethylamino) ethyl]-, 4-[2-(piperidin-1-yl)ethyl]-, 4-[3-(dimethylamino)propyl]- and 4-[2-hydroxy-3-(propan- 2-ylamino)propyl]- derivatives of 1,7-diethyl-8,9-diphenyl-4-azatricyclo[5.

Synthesis and in vitro cytotoxicity of cross-conjugated prostaglandin A and J series and their hydroxy derivatives.

The synthesis of two cross-conjugated prostaglandin analogues of known neurotrophic activity and their new hydroxy derivatives was accomplished starting from the diastereoisomeric (+)-camphor protected 3-[(dimethoxyphosphoryl)methyl]-4,5-dihydroxycyclopent-2-enones. The cytotoxicity of these compounds was determined against HeLa, K562, HL-60 human cancer cell lines and normal human cells (HUVEC). We found that NEPP11 and its C7-hydroxy derivative demonstrated high anticancer activity against the HeLa and HL-60 human cancer cell lines at concentrations ranging from 1 to 2 μM.

Chelating ability and biological activity of hesperetin Schiff base.

Hydrazone hesperetin Schiff base (HHSB) - N-[(±)-[5,7-dihydroxy-2-(3-hydroxy-4-methoxy-phenyl)chroman-4-ylidene]amino]benzamide has been synthesized and its crystal structure was determined. This compound was used for the formation of Cu(II) complexes in solid state and in solution which were characterized using different spectroscopic methods. The analyses of potentiometric titration curves revealed that monomeric and dimeric complexes of Cu(II) are formed above pH7.

Synthesis and cytotoxic properties of halogen and aryl-/heteroarylpiperazinyl derivatives of benzofurans.

A series of seven derivatives of 1,1'-(5,6-dimethoxy-3-methyl-1-benzofuran-2,7-diyl)diethanone was synthesized and characterized by (1)HNMR and ESI MS spectra and elemental analyses. The obtained new compounds and three halogen derivatives of benzofuran, reported in our earlier work, were tested for their cytotoxic properties in human chronic (K562) and acute (HL60) leukemia cells, human cervical cancer (HeLa), and normal endothelial cells (HUVEC). Four compounds (2, 3, 4, 5), which contain halogens in their structure showed significant anticancer activity.

N-Acyl-phosphoramidates as potential novel form of gemcitabine prodrugs.

Gemcitabine (dFdC) is a cytidine analog remarkably active against a wide range of solid tumors. Inside a cell, gemcitabine is phosphorylated by deoxycytidine kinase to yield gemcitabine monophosphate, further converted to gemcitabine di- and triphosphate. The most frequent form of acquired resistance to gemcitabine in vitro is the deoxycytidine kinase deficiency.

Synthesis and biological activity of novel series of 1,3-benzoxazol-2(3H)-one derivatives.

In the search for novel biological agents, a series of new derivatives N-substituted 1,3-benzoxazol-2(3H)-one, 5-chloro-1,3-benzoxazol-2(3H)-one, 6-bromo-1,3-benzoxazol-2(3H)-one were prepared. All of the compounds were characterized by 1H NMR, 13C NMR and ESI MS spectra. Moreover, for compound 1 an Xray structure was determined.

Design, synthesis and cytotoxicity of a new series of isoxazolidines derived from substituted chalcones.

A new series of isomeric isoxazolidin-3-yl-3-phosphonates were synthesised from N-methyl-C-diethoxyphosphorylnitrone and substituted chalcones. The respective isoxazolidin-3-yl-3-phosphonic acids were obtained from phosphonates via dealkylation procedure using trimethylsilyl bromide. Selected phosphonates and their respective phosphonic acids were screened for their cytotoxic activity to HeLa and K562 cells with IC(50) in the 0.

Design, synthesis and cytotoxicity of a new series of isoxazolidine based nucleoside analogues.

5-Arylisoxazolidin-3-yl-3-diethoxyphosphonates have been synthesized from N-methyl-C-diethoxyphosphorylnitrone and vinyl aryls in good yields and their transformation into the respective phosphonic acids has been accomplished via dealkylation procedure using trimethylsilyl bromide. Phosphonates having 1- and 2-naphthyl substituents at C5 in the isoxazolidine ring as well as the respective phosphonic acids have been found cytotoxic to HeLa and K562 cells with IC(50) in the 0.1-0.

(1→3)-β-D-Glucan inhibits a dual mechanism of peroxynitrite stroke.

Aim: The antioxidative and antinitrative activities of (1→3)-β-D-glucan (1-4μg/ml) from the yeast cell walls of Saccharomyces cerevisiae in human plasma treated with strong oxidants - peroxynitrite (ONOO(-)) (0.1mM) and hydrogen peroxide (H(2)O(2)) (2mM) were studied in vitro. The main purpose of this study was to assess if (1→3)-β-D-glucan, a well known strong immunostimulatory agent, possesses a protective function against dual mechanism of ONOO(-) stroke associated with nitrative and oxidative damages to human plasma biomolecules.

beta-glucan from Saccharomyces cerevisiae as a blood platelet antioxidant.

Blood platelets in addition to their haemostatic role can function as inflammatory cells. The aim of our study was to assess if beta-D-glucan, the natural, very strong biological response modifier, may protect platelet proteins and lipids against oxidative/nitrative damages. The antioxidative activity of the beta-D-glucan, a known immunomodulator derived from the yeast cell walls of species such as Saccharomyces cerevisiae, on blood platelets treated with oxidants-peroxynitrite and hydroperoxide-was studied in vitro.

Response of blood platelets to beta-glucan from Saccharomyces cerevisiae.

The effects of the beta-D-glucan, a polysaccharide derived from the yeast cell walls of species such as Saccharomyces cerevisiae, on blood platelets activation induced by physiological agonists (thrombin, ADP, collagen) in vitro were studied. The aim of our study was to assess in vitro if beta-glucan, a naturally strong biological response modifier, may modify platelet activation, i.e.