Search results for "Heterocyclic Compounds"
showing 10 items of 374 documents
Synthesis and biological evaluation of a D-ring-contracted analogue of lamellarin D
2017
A D-ring contracted analogue of the strongly cytotoxic marine pyrrole alkaloid lamellarin D was synthesized and investigated for its antiproliferative action towards a wild type and a multidrug resistant (MDR) cancer cell line. The compound was found to inhibit tumor cell growth at submicromolar concentrations and showed a lower relative resistance in the MDR cell line than the antitumor drug camptothecin to which lamellarin D shows cross resistance and with which lamellarin D shares the same binding site.
From anti-fouling to biofilm inhibition: New cytotoxic secondary metabolites from two Indonesian Agelas sponges
2010
Chemical investigation of Indonesian marine sponges Agelas linnaei and A. nakamurai afforded 24 alkaloid derivatives representing either bromopyrrole or diterpene alkaloids. A. linnaei yielded 16 bromopyrrole alkaloids including 11 new natural products with the latter exhibiting unusual functionalities. The new compounds include the first iodinated tyramine-unit bearing pyrrole alkaloids, agelanesins A-D. These compounds exhibited cytotoxic activity against L5178Y mouse lymphoma cells with IC(50) values between 9.25 and 16.76 muM. Further new compounds include taurine acid substituted bromopyrrole alkaloids and a new dibromophakellin derivative. A. nakamurai yielded eight alkaloids among th…
The translocation of signaling molecules in dark adapting mammalian rod photoreceptor cells is dependent on the cytoskeleton.
2008
In vertebrate rod photoreceptor cells, arrestin and the visual G-protein transducin move between the inner segment and outer segment in response to changes in light. This stimulus dependent translocation of signalling molecules is assumed to participate in long term light adaptation of photoreceptors. So far the cellular basis for the transport mechanisms underlying these intracellular movements remains largely elusive. Here we investigated the dependency of these movements on actin filaments and the microtubule cytoskeleton of photoreceptor cells. Co-cultures of mouse retina and retinal pigment epithelium were incubated with drugs stabilizing and destabilizing the cytoskeleton. The actin a…
S-Methylisothioharnstoffe, Bausteine kettenverzweigter Cimetidin-DerivateS-Methylisothioureas, Synthons for Chain-Branched Cimetidine Derivates
1987
A partir de S,S-dimethyl N-cyano dithiocarbonimidate et d'amino-2' alkyl (ramifie) thiomethyl-4 methyl-5 imidazoles (A), synthese des derives de A substitues sur l'amino-2' par [cyanoimino methylthiomethyle]
Selective, Sensitive, and Rapid Analysis with Lateral-Flow Assays Based on Antibody-Gated Dye-Delivery Systems: The Example of Triacetone Triperoxide
2013
[EN] Antibodygated MSNs that are loaded with a rhodamine dye and that can be used for the determination of the presence of peroxide-based explosive TATP with a lateral-flow fluorescence reader have been designed and prepared, thereby allowing for detection limits in the lower ppb range. The mechanism of the detection relies on a displacement of the antibody from the surface of the hybrid material because of highly affine antibody-TATP interactions, which release a much larger number of entrapped dye molecules from the pores than antibodies are displaced. The high selectivity of the antibody is retained in the gated material, thus allowing for a remarkable discrimination against H2O2. System…
Stereoselective synthesis of 2-amino-1-hydroxy-3-phenylpropylphosphonic acid
1996
Abstract A highly stereoselective synthesis of 2-amino-1-hydroxy-3-phenylpropylphosphonic acid was achieved by simple addition of diethyl phosphite to enantiomeric N-blocked phenylalaninals. These compouds exhibit significant herbicidal activity.
ChemInform Abstract: Stereoselective Synthesis of 2-Amino-1-hydroxy-3- phenylpropylphosphonic Acid.
2010
Abstract A highly stereoselective synthesis of 2-amino-1-hydroxy-3-phenylpropylphosphonic acid was achieved by simple addition of diethyl phosphite to enantiomeric N-blocked phenylalaninals. These compouds exhibit significant herbicidal activity.
Zidovudine (AZT) causes an oxidation of mitochondrial DNA in mouse liver
1999
Zidovudine (3′-azido-2′,3′-dideoxythymidine [AZT]) inhibits human immunodeficiency virus replication and delays progression of acquired immune deficiency syndrome. We have recently found that, in muscle, AZT causes oxidative damage to mitochondrial DNA (mtDNA) and other signs of mitochondrial oxidative damage. The aim of this work was to test if AZT causes oxidative damage to liver mtDNA. In our study, an experimental mouse model was used in which mice were administered AZT (10 mg/kg body weight/d) in drinking water. Liver mtDNA of mice treated with AZT had 40% more of the oxidized, mutagenic nucleoside, 8-oxo-7,8-dihydroxy-2′deoxyguanosine (8-oxo-dG) than untreated controls. This oxidative…
Synthesis of a New Fluorinated Oxazolidinone and Its Reactivity as a Chiral Auxiliary in Aldol Reactions.
2007
A new enantiomerically pure fluorinated oxazolidinone has been prepared from a fluorinated imidoyl chloride and an optically pure sulfoxide. The diastereoselective reduction of the β-iminosulfoxide thus formed followed by elimination of the sulfoxide and cyclization of the created aminoalcohol furnishes the desired product. The fluorinated oxazolidinone was subsequently used as a chiral auxiliary in Aldol reactions. We also found that the selective formation of the syn-Evans and syn-non-Evans diastereoisomer can be controlled by adjusting the Lewis acid/base ratio.
Determination of 2,3,7,8-tetrachlorodibenzo-p-dioxin in goat milk and tissues by glass capillary gas chromatography and medium resolution mass fragme…
1981
Abstract An analytical method has been developed for the study of the elimination of 2,3,7,8-tetrachlodoribenzo-p-dioxin (TCDD) by lactation and its determination in various tissues of goat. The method is based on the alkaline hydrolysis of milk, liver, fat, muscle, blood, faeces and urine samples, extraction with n-hexane, treatment with sulphuric acid-saturated silica gel, chromatographic clean-up on silica gel and alumina micro-columns, and glass capillary gas chromatography—medium resolution mass fragmenography (resolution 2000). 1,2,3,4-Tetrachlorodibenzo-p-dioxin is used as the internal standard, the concentration of TCDD being determined from the calibration curve calculated from the…