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1.
Nat Commun ; 13(1): 6620, 2022 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-36333309

RESUMO

As we approach the era of quantum advantage, when quantum computers (QCs) can outperform any classical computer on particular tasks, there remains the difficult challenge of how to validate their performance. While algorithmic success can be easily verified in some instances such as number factoring or oracular algorithms, these approaches only provide pass/fail information of executing specific tasks for a single QC. On the other hand, a comparison between different QCs preparing nominally the same arbitrary circuit provides an insight for generic validation: a quantum computation is only as valid as the agreement between the results produced on different QCs. Such an approach is also at the heart of evaluating metrological standards such as disparate atomic clocks. In this paper, we report a cross-platform QC comparison using randomized and correlated measurements that results in a wealth of information on the QC systems. We execute several quantum circuits on widely different physical QC platforms and analyze the cross-platform state fidelities.

2.
Farmaco ; 59(4): 297-305, 2004 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15081347

RESUMO

The multistep synthesis of a series of new substituted-benzothiazoles as hydrochloride or quaternary salts is described. 6-Amidino substituted 2-aminobenzothiazoles (5, 6), N-methyl-2-(4-cyanostyryl)benzothiazolium iodide (8), cyano-substituted-2-styrylbenzothiazoles (9-11) and amidino and bis-amidino-substituted 2-styrylbenzothiazoles (12-17) were prepared. The crystal structure of amidino derivative (6) was determined by single crystal X-ray analysis. All new prepared compounds were tested on the cytostatic activities against malignant cell lines: (SW620, colon carcinoma; Hep2, laryngeal carcinoma; HBL, melanoma; HeLa, cervical carcinoma and WI38, human normal fibroblasts). The compounds exerted a different inhibitory effect, depended on concentration and type of the cells. The best inhibitory effect was achieved with compounds (12-15), with slight differences among them. All of them inhibited the growth of examined tumor cell lines and also normal fibroblasts. Other examined compounds exhibited a moderate inhibitory effect, depending on type of the cells. Majority of them inhibited the growth of HeLa cells and WI38.


Assuntos
Inibidores do Crescimento/síntese química , Inibidores do Crescimento/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Benzotiazóis , Divisão Celular/efeitos dos fármacos , Divisão Celular/fisiologia , Linhagem Celular , Linhagem Celular Tumoral , Cristalização , Cristalografia por Raios X/métodos , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos/métodos , Fibroblastos/citologia , Fibroblastos/efeitos dos fármacos , Inibidores do Crescimento/química , Células HeLa , Humanos , Tiazóis/química
3.
Eur J Med Chem ; 46(7): 2770-85, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21524828

RESUMO

We report on the synthesis of the novel types of cytosine and 5-azacytosine (1-9), uracil and 6-azauracil (13-18) and cyanuric acid (19-22) derivatives of l-ascorbic acid, and on their cytostatic activity evaluation in human malignant tumour cell lines vs. their cytotoxic effects on human normal fibroblasts (WI38). The CD spectra analysis revealed that cytosine (5 and 6), uracil (14-16), 6-azauracil (17) and cyanuric acid (21) derivatives of l-ascorbic acid bearing free amino group at ethylenic spacer existed as a racemic mixture of enantiomers, whereas L-ascorbic derivatives containing the C-5 substituted hydroxy group at the ethylenic spacer were obtained in (4R, 5S) enantiomeric form. The stereochemistry of 6-azauracil derivative of l-ascorbic acid (13) was confirmed by X-ray crystal structure analysis. The molecules are self-assembled by one N-H⋯O hydrogen bond, two C-H⋯O hydrogen bonds and two C-H⋯π interactions into three-dimensional framework. Cytostatic activity evaluation indicated that compounds did not show distinctive antiproliferative effects on tested cell line panel. However, the cytosine derivative of l-ascorbic acid (1) containing the C4-C5 double bond conjugated with the lactone moiety produced rather marked growth inhibitory effect on hepatocellular carcinoma (HepG2), metastatic breast epithelial carcinoma (MCF-7) and cervical carcinoma (HeLa) cell lines at micromolar concentrations, but also exerted strong cytostatic effect on WI38. 5-Azacytosine derivative of l-ascorbic acid (2) with a double bond at the C4-C5 conjugated with the lactone moiety displayed potent antitumour activity against tested tumour cell lines with meanIC(50) values ranging from 0.92 to 5.91 µM. However, this compound also exhibited pronounced cytotoxicity towards WI38. Flow cytometric analysis of the cell cycle revealed that compound 2 triggers S phase arrest, which clearly demonstrates its interference with DNA replication, a key event of cell proliferation. Marked anticancer efficacy of compound 2 supports further in vivo investigation into its possible clinical utility.


Assuntos
Ácido Ascórbico/síntese química , Citosina/síntese química , Citostáticos/síntese química , Triazinas/síntese química , Uracila/síntese química , Ácido Ascórbico/farmacologia , Linhagem Celular , Cristalografia por Raios X , Citosina/análogos & derivados , Citosina/farmacologia , Citostáticos/farmacologia , Fibroblastos , Células HeLa , Células Hep G2 , Humanos , Ligação de Hidrogênio , Concentração Inibidora 50 , Células MCF-7 , Pontos de Checagem da Fase S do Ciclo Celular/efeitos dos fármacos , Estereoisomerismo , Relação Estrutura-Atividade , Triazinas/farmacologia , Uracila/análogos & derivados , Uracila/farmacologia
4.
Opt Lett ; 31(6): 757-9, 2006 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-16544614

RESUMO

We demonstrate an ultraviolet diode laser system for cooling of trapped ytterbium ions. The laser power and linewidth are comparable to those of previous systems based on resonant frequency doubling, but the system is simpler, more robust, and less expensive. We use the laser system to cool small numbers of ytterbium ions confined in a linear Paul trap. From the observed spectra, we deduce final temperatures of < 270 mK.

5.
J Pept Res ; 66(2): 85-93, 2005 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-16000122

RESUMO

The novel hydroxyurea 5 derivative of L-valine was prepared by aminolysis of N-(1-benzotriazolecarbonyl)-L-valine cyclohexanemethylamide 4 with hydroxylamine. The corresponding hydantoin derivative 6 was synthesized by base catalyzed cyclization of the amide 4. The exact stereostructure of hydantoin derivative 6 has been determined by X-ray crystal structure analysis. The chiral atom of the hydantoin ring in 6 has S configuration what is in agreement with its configuration in the starting L-valine. The molecules of 6 are joined into infinite chains by N-H...O intermolecular hydrogen bond. The infinite chains are additionally linked by two C-H...O hydrogen bonds, thus forming two-dimensional network. The hydantoin derivative of L-valine 6 and its L-leucine analogue LH have similar packing arrangements, so they are homostructural.


Assuntos
Hidantoínas/química , Hidroxiureia/análogos & derivados , Hidroxiureia/química , Valina/química , Cristalografia por Raios X , Hidantoínas/síntese química , Hidantoínas/farmacologia , Ligação de Hidrogênio , Hidroxiureia/síntese química , Hidroxiureia/farmacologia , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-Atividade
6.
J Pept Res ; 63(5): 391-8, 2004 May.
Artigo em Inglês | MEDLINE | ID: mdl-15140156

RESUMO

The novel purine and pyrimidine derivatives of 1-aminocyclopropane-1-carboxylic acid 1 and 2 were obtained by alkylation of 6-(N-pyrrolyl)purine and thymine with methyl 1-benzamido-2-chloromethylcyclopropanecarboxylate. X-ray crystal structure analysis shows that the cyclopropane rings in 1 and 2 posses Z-configuration. The cyclopropane ring atoms and attached atoms of the benzamido and methoxycarbonyl moiety of both molecules are disposed perpendicularly to each other. The carbonyl oxygen of the methoxycarbonyl moiety adopts in both compounds a synperiplanar conformation with respect to the midpoint of the distal bond of the cyclopropane ring. The torsion angles Phi and psi for the 1-aminocyclopropane-1-carboxylic acid residue in 1 and 2 correspond to a folded conformation, while the torsion angles omega define antiperiplanar conformation. Intermolecular hydrogen bonds connect the molecules of 1 into dimers. Each dimer is hydrogen-bonded with four ethanol molecules, thus forming discrete unit. On the contrary, intermolecular hydrogen bonds link the molecules of 2 generating three-dimensional network.


Assuntos
Aminoácidos Cíclicos/síntese química , Modelos Moleculares , Purinas/química , Timina/química , Aminoácidos Cíclicos/química , Cristalografia por Raios X , Ligação de Hidrogênio , Estrutura Molecular
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