Search results for "DISCOVERY"
showing 10 items of 4119 documents
Antineoplastika, 19. Mitt.: Darstellung vonN-[2-Chlor-4-diethylamino-(1,3,5-triazin-6-yl)]-aminosäuren
1990
Multidrug resistance reverting activity and antitumor profile of new phenothiazine derivatives
2008
Abstract A series of easily affordable phenothiazine derivatives bearing a rigid but-2-ynyl amino side chain were synthesized and tested to evaluate the MDR reverting activity and full antitumor profile. Some compounds endowed with remarkable MDR reverting effect were identified, and the most active one ( 6c ) was shown to increase doxorubicin retention in multidrug resistant cells, suggesting a direct interaction with P-glycoprotein. Furthermore, a broad range of cellular activities were observed for different compounds. In particular, the ability of some derivatives to induce antiproliferative effects on resistant cell lines and to interfere with the G 1 phase of the cell cycle, a phase u…
New propylamine oligopyrrole carboxamides linked to a heterocyclic or anthraquinone system: synthesis, DNA binding, topoisomerase I inhibition and cy…
2003
Continuing our studies on combilexines, compounds consisting of a DNA intercalator linked to a minor groove ligand, new results are presented. The synthesis of a series of new propylamine oligopyrrole carboxamides closely related to netropsin and distamycin A, linked to a heterocyclic or anthraquinone system is reported. The cytotoxic activity in vitro, the DNA binding characteristics and the inhibition of the topoisomerase I of the compounds were studied in order to explain the biological mechanism of action of these new potential combilexines. Some of the synthesised compounds showed cytotoxic activity against human tumour cell lines, as well as DNA binding and topoisomerase I inhibiting …
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
2003
A series of 2,3-disubstituted indenes, which are analogues of the widely used histamine H(1) receptor antagonist dimethindene, have been synthesized and studied as muscarinic and histamine receptor antagonists. The affinities of these compounds for the five human muscarinic receptor subtypes (M(1)-M(5)) and for human histamine H(1) receptors were determined in radioligand binding studies using membranes from transfected Chinese hamster ovary (CHO) cells and [(3)H]N-methylscopolamine ([(3)H]NMS). The results demonstrate that the diisopropyl analogue 19 has a similar high affinity as (S)-dimethindene at M(2) receptors ((S)-dimethindene: pK(i) = 7.52; (-)-19: pK(i) = 7.37) with an improved sel…
Aldol Reactions with Erythrulose Derivatives: Stereoselective Synthesis of Differentially Protected syn -α,β-Dihydroxy Esters
2000
Boron enolates of 1-O-silylated erythrulose 3,4-acetonides prepared with Brown's chloro-dicyclohexylborane/tertiary amine system have been shown to react with achiral aldehydes in a highly stereoselective way to yield a 1,2-syn/1,3-syn stereoisomer. Through oxidative cleavage of the aldol adducts with periodic acid hydrate, enantiopure syn-α,β-dihydroxy esters with either hydroxyl group differently protected have been prepared. These erythrulose derivatives therefore behave as a chiral hydroxy acetate (glycolate) enolate equivalent.
Effects of Propofol (Intravenous Propofol Emulsion) on Cell Membranes Measured by Electrofusion and Electroporation
2011
The influence of propofol (CAS 2078-54-8 (intravenous propofol emulsion) on cell membrane properties was investigated in vitro with techniques of cell electrofusion and cell electroporation. Human lymphoma cells and plant protoplasts were chosen as a model system. Propofol (intravenous propofol emulsion) decreased the electrofusion yield of the cells and their membrane permeability. A 50% decrease in relative electrofusion was observed in human lymphoma cells in the presence of about 0.05 mmol/l propofol (intravenous propofol emulsion) and in plant protoplasts in the presence of about 0.1 mmol/l. The fusion of human lymphoma cells was inhibited to 100% at concentrations higher than 0.2 mmol…
Cytotoxic phytochemicals from the crude extract of Tetrapleura tetraptera fruits towards multi-factorial drug resistant cancer cells.
2020
Abstract Ethnopharmacological relevance Tetrapleura tetraptera is an African medicinal spice used in traditional medicine to treat several ailments including cancer. Aim of the study The present study was designed to evaluate the cytotoxicity of the dichloromethane-methanol (1:1) extract of the fruits of Tetrapleura tetraptera (TTF) and its constituents: (3R, 4S)-3,4-dimethyloxetan-2-one (1), luteolin (2), stigmasterol (4), 3-O-[6′-O-undecanoyl-β-D-glucopyranosyl]stigmasterol (6), olean-12-en-3-β-O-D-glucopyranoside (7), 3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosylurs-12-en-28-oic acid (8), 3-O-β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranosyl-27-hydroxyolean-12-ene-28-oic acid (9), methyl…
2-Hydroxyoleic Acid Induces ER Stress and Autophagy in Various Human Glioma Cell Lines
2012
Background: 2-Hydroxyoleic acid is a synthetic fatty acid with potent anti-cancer activity which does not induce undesired side effects. However, the molecular and cellular mechanisms by which this compound selectively kills human glioma cancer cells without killing normal cells is not fully understood. The present study was designed to determine the molecular bases underlying the potency against 1321N1, SF-767 and U118 human glioma cell lines growth without affecting non cancer MRC-5 cells. Methodology/Principal Findings: The cellular levels of endoplasmic reticulum (ER) stress, unfolded protein response (UPR) and autophagy markers were determined by quantitative RT-PCR and immunoblotting …
The metabolic syndrome and HIV infection.
2013
The metabolic syndrome (MetS), a cluster of risk factors for cardiovascular disease and type 2 diabetes, has become an important public health problem. Considerable differences in the prevalence of the MetS in human immunodeficiency virus (HIV)-infected subjects have been reported, as a consequence of several limitations regarding the diagnostic critera for MetS. New evidence suggests that the use of optimal waist cut-off points specific for the various ethnic populations could represent a step forward in overcoming these limitations. Also the use of specific cut-off points for measuring upper trunk fat as an adjunctive criterion of MetS in HIV patients with lipodystrophy could represent an…
La scoperta, sistemazione e conservazione della grande Iscrizione di Gortina, nell'isola di Creta (1884-1921): la protezione delle testimonianze e le…
2013
La scoperta e la conservazione della Grande Iscrizione di Gortina a Creta, da parte degli studiosi italiani, fra la fine del XIX sec. e i primi decenni del XX sec., rappresentò un grande riconoscimento scientifico-culturale per la giovane nazione italiana. Nel passato, l’isola di Creta era stata legata alla Repubblica di Venezia e anche questo rapporto favorì l’invio a Creta del giovane epigrafista F. Halbherr, il quale fra notevoli peripezie rinvenne, assieme all’epigrafista tedesco E. Fabricius, la famosa l’iscrizione nell’antica città di Gortina. L’iscrizione, fra le più antiche e complete finora conosciute in tutta Europa, conteneva le norme sulla famiglia, l’eredità e in generale i dir…