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71.
Károlyi BI Bösze S Orbán E Sohár P Drahos L Gál E Csámpai A 《Molecules (Basel, Switzerland)》2012,17(3):2316-2329
A series of novel functionalized mono-, bis- and tris-(S)-{[(2S,4R,8R)-8-ethyl-quinuclidin-2-yl](6-methoxyquinolin-4-yl)}methanamines including ferrocene-containing derivatives was obtained by the reaction of the precursor amine with a variety of acylation agents. Their in vitro antitumor activity was investigated against human leukemia (HL-60), human neuroblastoma (SH-SY5Y), human hepatoma (HepG2) and human breast cancer (MCF-7) cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)-assay and the 50% inhibitory concentration (IC(50)) values were determined. Our data indicate that the precursor amine has no antitumor activity in vitro, but the bis-methanamines with ureido-, thioureido and amide-type linkers display attractive in vitro cytotoxicity and cytostatic effects on HL-60, HepG2, MCF-7 and SH-SY5Y cells. Besides 1H- and 13C-NMR methods the structures of the new model compounds were also studied by DFT calculations. 相似文献
72.
ortho-Nitrophenyl-substituted condensed 1,3-benzothiazines proved to be a useful core unit in indole syntheses under non-reductive conditions. Thus, the treatment of ortho-nitro-2-aryl-2a-chloro-4H-azeto[2,1-b][1,3]benzothiazin-1-ones with sodium methoxide in methanol provided indolo-1,4-benzothiazepines via a novel rearrangement. Through the sulfur extrusion reaction of indolo[2,3-b][1,4]benzothiazepines, further alkaloid-type indole derivatives, indolo[3,2-c]isoquinolines, were obtained. The structures of the new ring systems were determined by means of NMR spectroscopy. 相似文献
73.
L de Lichtervelde CE Antal AE Boitano Y Wang P Krastel F Petersen AC Newton MP Cooke PG Schultz 《Chemistry & biology》2012,19(8):994-1000
To identify small molecules that selectively control hematopoietic stem cell differentiation, we performed an unbiased screen using primary human CD34(+) cells. We identified a plant-derived natural product, euphohelioscopin A, capable of selectively differentiating CD34(+) cells down the granulocyte/monocytic lineage. Euphohelioscopin A also inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60. Mechanistic studies revealed that euphohelioscopin A is an activator of protein kinase C (PKC), and that the promonocytic effects of this natural product are mediated by PKC activation. In addition to shedding insights into normal hematopoiesis, this work may ultimately facilitate the application of stem cell therapies to a host of myeloid dysfunctions. 相似文献
74.
Viktor Háda Antal Tungler László Szepesy 《Reaction Kinetics and Catalysis Letters》2001,73(1):109-115
High diastereoselectivities were obtained in the heterogeneous catalytic hydrogenation of chiral pyrrole and pyridine derivatives with complete conversion, in non-acidic medium. The products of the hydrogenations, secondary and tertiary amines act as catalyst modifiers, increasing the d.e. values in the last period of the reactions. 相似文献
75.
JPC – Journal of Planar Chromatography – Modern TLC - 相似文献
76.
Low-spin levels in 136Ba have been studied by means of the (n, n'γ) reaction using reactor fast neutrons. Excited states up to an excitation energy of 2.8 MeV and with spin values up to 7 were found to be populated. Energies, intensities and angular distributions of γ-rays attributed to 136Ba have been measured.In addition to the confirmation of known level characteristics the angular distribution data resulted in new unique spin assignments for 7 levels (2 for the levels at 2080.0 keV, 2128.8 keV and 2484.7keV, 3 for those at 2390.8, 2399.8 and 2431.0 keV as well as 0+ for the 2141.3 keV level). Furthermore E2/M1 multipole mixing ratios were determined for the most intensive mixed γ-transitions. 相似文献
77.
R. Antalík 《Czechoslovak Journal of Physics》1991,41(5):427-440
We investigate the dependence of the neutron-proton matrix element ratios (η) on radial neutron and proton ground state density distribution differences (Δ np) within the framework of the shell model quasiparticle random phase approximation. We show that theη ratios are linearly dependent onΔ rms np differences. We prove the consistency of empirical and theoretical methods by agreement of theη ratios obtained from the 1 GeV proton inelastic scattering analysis and from the QRPA calculations. 相似文献
78.
The numbers are twin primes.
79.
Pál?SohárEmail author Antal?Csámpai Gábor?Magyarfalvi Angela E.?Szabó Géza?Stájer 《Monatshefte für Chemie / Chemical Monthly》2004,135(12):1519-1527
Summary. t-2-Benzoyl-t-4-phenylcyclohexane-r-1-carboxylic acid reacts with hydrazine to give the saturated 1,7-diphenyl-trans-phthalazin-4(3H)-one. The reaction of the acid with ethylenediamine yields diastereomeric trans-imidazo[2,3-a]isoindoles, which differ in their C-1 configuration. The cyclizations of the acid with cis-2-aminocyclohexane- or 4-cyclohexenemethanol result in trans-isoindolo[2,1-a][3,1]benzoxazines, while in its reactions with the analogous di-endo- and di-exo-norbornane- and -norborneneamino alcohols, the acid gives methylene-bridged isomeric di-endo-norbornanes or a norbornene derivative; the corresponding diastereomeric di-exo derivatives have also been prepared. After isolation, the structures were established by means of 1H and 13C NMR spectroscopy, with application of DIFFNOE, DEPT, HMQC, HMBC, and 2D-COSY techniques. 相似文献
80.
Péter A Arki A Vékes E Tourwé D Lázár L Fülöp F Armstrong DW 《Journal of chromatography. A》2004,1031(1-2):171-178
Direct and indirect reversed-phase (RP) high-performance liquid chromatographic methods were developed for the separation of enantiomers of 18 unnatural beta-amino acids, including several beta-3-homo amino acids. The direct separations of the underivatized analytes were performed on chiral stationary phases (CSPs) containing macrocyclic glycopeptide antibiotic teicoplanin (Chirobiotic T column) and teicoplanin aglycone (Chirobiotic TAG column). The indirect method involved pre-column derivatization with a new chiral derivatizing agent (CDA), (S)-N-(4-nitrophenoxycarbonyl)phenylalanine methoxyethyl ester ((S)-NIFE), and subsequent separation of diastereomers on Discovery C18 and Hyperpep 300 C18 columns. The different methods were compared in systematic chromatographic examinations. The effects of organic modifier, mobile phase composition, pH and flow rate on the separation were investigated. 相似文献