171 research outputs found

    Multicomponent and 1,3-dipolar cycloaddition synthesis of triazole- and isoxazole-acridinedione/xanthenedione heterocyclic hybrids: cytotoxic effects on human cancer cells

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    A new series of diverse 1,2,3-triazole-acridinedione/xanthenedione and 1,2-isoxazole-acridinedione/xanthenedione heterocyclic hybrids have been synthesized via 1,3-dipolar coupling reaction of N/O-substituted-acridinedione-alkyne or O-substituted-xanthenedione-alkyne substrates with various aromatic azides or oximes. In all cases, the cycloaddition is totally regioselective. The chemical structures of the synthesized compounds are determined using 2D NMR and are further confirmed by single-crystal X-ray diffraction analysis. Preliminary in vitro cytotoxic assays on two human breast cancer cell lines (MDA-MB-231, T47-D) and one prostate cancer cell line (PC3) are performed on some selected compounds. The most active O-1,2,3-triazole-xanthenedione hybrid displays the best cytotoxicity effects with IC50 ≤ 20 μM in breast cancer and IC50 = 10 μM in prostate cancer cell lines.publishe

    A step-by-step synthesis of triazole-benzimidazole-chalcone hybrids: Anticancer activity in human cells+

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    Novel series of triazole-benzimidazole-chalcone hybrid compounds have been synthesized via click chemistry, between different azide derivatives and substituted benzimidazole terminal alkynes bearing a chalcone moiety. The starting alkynes are prepared via base-catalysed nitrogen alkylation of pre-synthetized benzimidazole-chalcone substrates. All the intermediates as well as the final products are fully characterized by 1D and 2D NMR and mass spectrometry techniques. HMBC correlations permits the identification of a unique 1,4-disubstitued triazole-benzimidazole-chalcone isomer. Evaluation of the anti-proliferative potential in breast and prostate cancer cell lines showed that the presence of chloro substituents at the chalcone ring of the triazole-benzimidazole-chalcone skeleton enhanced the cytotoxic effects. The benzyl group linked to the 1,2,3-triazole moiety provides more antiproliferative potential.publishe

    Water requirements and single and dual crop coefficients of sugarcane grown in a tropical region, Brazil

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    A field experiment was conducted throughout 2009/2010 in a sugarcane field of a commercial distillery located on the coastal area of Paraiba state, Brazil. The objectives were to determine sugarcane water requirements and to test the single and dual crop coefficients by comparing the calculated values of ET with measured ones. Crop evapotranspiration was determined by field water balance, reference evapotranspiration (ETo) by the Penman-Monteith approach, while single and dual crop coefficients were computed through the standard FAO-56 methodology. The experi- mental area was cultivated with irrigation ap-plied weekly by a centre pivot system in addition to rainfall and the irrigation scheduling was based on 100% ETo. Three statistical tests, mean bias difference (MBD), normalized root mean square difference (NRMSD) and regression analysis, were used to evaluate the performance of single and dual crop coefficients. Results showed that there was a notable symmetry between ET meas- ured and ET calculated by Kc dual. The ET val- ues, calculated from Kc single, underestimated those obtained from soil water balance meas- urements by 36%

    Comportamento de dois genótipos de milho cultivados em sistema de aléias preestabelecido com diferentes leguminosas arbóreas.

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    O cultivo em aléias tem sido recomendado como alternativa para a substituição da agricultura de corte e queima, no trópico úmido, devido à grande capacidade de produção de matéria orgânica e de reciclagem de nutrientes, mas algumas dúvidas quanto à sustentabilidade e à competição interespecífica são persistentes. O objetivo no trabalho foi avaliar a viabilidade da cultura do milho em um sistema de cultivo em aléias de leguminosas arbóreas. O delineamento experimental utilizado foi em blocos casualisados, com quatro repetições dos tratamentos: aléias de sombreiro (Clitoria fairchildiana), ingá (Inga edulis), guandu (Cajanus cajan) e leucena (Leucaena leucocephala) e uma testemunha sem aléias. Foram avaliadas a remobilização de carbono e nitrogênio, massa de grãos, massa de mil grãos e competição interespecífica entre as cultivares de milho e as leguminosas. A produção de grãos foi maior nas parcelas com C. fairchildiana e L. leucocephala. A produtividade do híbrido de milho foi superior à da variedade em todos os tratamentos. A produtividade e a massa de mil grãos de milho não são negativamente afetadas pela distância da linha da leguminosa arbórea. Esse estudo conclui que o sistema de aléias com leguminosas arbóreas é uma alternativa importante ao manejo sustentável dos agroecossistemas no tropico úmido. Além disso, nessa região a produtividade em grãos na cultura do milho é favorecida no sistema de aléias preeestabelecidas com as leguminosas arbóreas sombreiro, ingá e leucena e pela utilização de genótipos eficientes no aproveitamento do nitrogênio, cujo sincronismo entre a liberação e a absorção do N aplicado por meio das leguminosas deve ser aprimorado
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