1,394 research outputs found

    Controle de Sclerotinia sclerotiorum (L.) de Bary e Alternaria spp. em sementes de girassol Helianthus annuus (L.).

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    Cycloaddition of Benzyne with Alkoxy Substituted Pyrroline-N-oxides: Unexpected Rearrangement to a N-Phenylpyrrole

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    Reaction of enantiopure 3,4-dialkoxy-pyrroline N-oxides with benzyne affords the expected tetrahydrobenzo[d]pyrrolo[1,2-b]isoxazoles along with an unexpected 2,3-disubstitued-N-phenyl-pyrrole derived from an unprecedented rearrangement of the adduct of nitrone with two molecules of benzyne. A mechanism for the unusual rearrangement is proposed. The benzo[d]isoxazolidine derivatives are conveniently converted into 2-(2-hydroxyphenyl)-3,4-dialkoxypyrrolidines by reductive opening of the N–O bond.</jats:p

    Organised turbulence over mobile and immobile hydraulically rough boundaries

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    33rd IAHR Congress: Water Engineering for a Sustainable EnvironmentThe present work is aimed at the study of near-bed organised turbulence over mobile and immobile, porous, hydraulically rough boundaries. The bed was permeable and composed of non-cohesive sediments. Two data sets were analysed, characterised by the same u*. The mobile bed data featured generalised sediment transport for all size fractions smaller than the d90. The fixed bed was obtained as result of an armouring process. Comparison of these data sets reveals differences on such parameters of the bursting cycle as the maximum shear stress and the transported momentum. These results point to a reorganization of turbulence, in the near-bed region, when the bed is mobile. The impacts of these reorganization are discussed, namely in what concerns the third order moments of the distributions of the velocity fluctuations

    BCR-ABL residues interacting with ponatinib are critical to preserve the tumorigenic potential of the oncoprotein

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    Patients with chronic myeloid leukemia in whom tyrosine kinase inhibitors (TKIs) fail often present mutations in the BCR-ABL catalytic domain. We noticed a lack of substitutions involving 4 amino acids (E286, M318, I360, and D381) that form hydrogen bonds with ponatinib. We therefore introduced mutations in each of these residues, either preserving or altering their physicochemical properties. We found that E286, M318, I360, and D381 are dispensable for ABL and BCR-ABL protein stability but are critical for preserving catalytic activity. Indeed, only a "conservative" I360T substitution retained kinase proficiency and transforming potential. Molecular dynamics simulations of BCR-ABLI360T revealed differences in both helix αC dynamics and protein-correlated motions, consistent with a modified ATP-binding pocket. Nevertheless, this mutant remained sensitive to ponatinib, imatinib, and dasatinib. These results suggest that changes in the 4 BCR-ABL residues described here would be selected against by a lack of kinase activity or by maintained responsiveness to TKIs. Notably, amino acids equivalent to those identified in BCR-ABL are conserved in 51% of human tyrosine kinases. Hence, these residues may represent an appealing target for the design of pharmacological compounds that would inhibit additional oncogenic tyrosine kinases while avoiding the emergence of resistance due to point mutations.This work was supported by an investigator grant to P.V. from Associazione Italiana per la Ricerca sul Cancro (AIRC) and by funding from the Biotechnology and Biological Sciences Research Council (BB/I023291/1 and BB/H018409/1 to AP and FF). P.B. is the recipient of an AIRC - Marie Curie fellowship

    Potencial de armazenamento de sementes de soja transgênica X convencional.

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    A soja Roundup Ready (RR) foi a primeira planta transgênica a ser aprovada para alimentação humana e animal para cultivo no Brasil. No caso da soja resistente ao glyphosate, a tolerância ao herbicida foi obtida pela inserção de um gene oriundo do genoma da Agrobacterium sp. Sob tratamento com esse herbicida, as plantas de soja não são afetadas, em virtude da ação continuada e sistemática dessa enzima alternativa, insensível ao produto. Porém, há relatos de decréscimo no potencial de armazenamento de sementes de soja transgênica, quando comparadas às convencionais. Neste trabalho o objetivo foi avaliar o potencial de armazenamento de sementes de variedades de soja transgênica (RR), comparativo a suas isolinhas não geneticamente modificadas. O potencial fisiológico (germinação e vigor - envelhecimento acelerado e emergência em areia) das variedades transgênicas foi analisado comparativamente com suas isolinhas em quatro períodos de armazenamento, com quatro repetições cada teste. As avaliações foram realizadas a cada dois meses. As variedades testadas foram BRS Valiosa RR e sua isolinha BR 46 Conquista; BRS 255 RR e BRS 137; BRS 245 RR e BRS 133. As variedades foram semeadas na mesma época e local, com o mesmo manejo cultural. Foi realizada capina manual, a colheita foi realizada em R7 e as plantas foram colocadas para secar a sombra. Após secas as vagens foram debulhadas manualmente. As sementes foram armazenadas em câmara refrigerada à temperatura de 18 ºC ± 2 ºC e 75% ± 4% de umidade relativa, até o momento da instalação dos experimentos. Não ocorreram variações nos potenciais de armazenamento entre as variedades transgênicas e suas isolinhas não geneticamente modificadas. O decréscimo do potencial fisiológico das sementes durante o armazenamento foi em função do qualidade inicial independente da variedade

    Palladium(II) complexes of quinolinylaminophosphonates: synthesis, structural characterization, antitumor and antimicrobial activity

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    Three types of palladium(II) halide complexes of quinolinylaminophosphonates have been synthesized and studied. Diethyl and dibutyl [alpha-anilino-(quinolin-2-ylmethyl)]phosphonates (L1, 12) act as N,N-chelate ligands through the quinoline and aniline nitrogens giving complexes cis-[Pd(L1/12)X-2] (X Cl, Br) (1-4). Their 3-substituted analogues [alpha-anilino-(quinolin-3-ylmethyl)]phosphonates (L3, L4) form dihalidopalladium complexes trans-[Pd(L3/L4)(2)X-2] (5-8), with trans N-bonded ligand molecules only through the quinoline nitrogen. Dialkyl [alpha-(quinolin-3-ylamino)-N-benzyl]phosphonates (L5, L6) give tetrahalidodipalladium complexes [Pd-2(L5/L6)(3)X-4] (9-12), containing one bridging and two terminal ligand molecules. The bridging molecule is bonded to the both palladium atoms, one through the quinoline and the other through the aminoquinoline nitrogen, whereas terminal ligand molecules are coordinated each only to one palladium via the quinoline nitrogen. Each palladium ion is also bonded to two halide ions in a trans square-planar fashion. The new complexes were identified and characterized by elemental analyses and by IR, UV-visible, H-1, C-13 and P-31 nuclear magnetic resonance and ESI-mass spectroscopic studies. The crystal structures of complexes 1-4 and 6 were determined by X-ray structure analysis. The antitumor activity of complexes in vitro was investigated on several human tumor cell lines and the highest activity with cell growth inhibitory effects in the low micromolar range was observed for dipalladium complexes 11 and 12 derived from dibutyl ester L6. The antimicrobial properties in vitro of ligands and their complexes were studied using a wide spectrum of bacterial and fungal strains. No specific activity was noted. Only ligands L3 and L4 and tetrahalidodipalladium complexes 9 and 11 show poor activities against some Gram positive bacteria

    The many roles of mellitic acid during barium sulfate crystallization

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    The various roles of mellitic acid during barium sulfate crystallization from nucleation to mesocrystal formation are explored and elucidated
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