Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-Aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors

The synthesis and biological evaluation of novel 1-aryl-3-[2-, 3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas 3, 4 and 5 as VEGFR-2 tyrosine kinase inhibitors, are reported. The 1-aryl-3-[3-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas 4a-4h, with the arylurea in the meta position to the thioether, showed the lowest IC50 values in enzymatic assays (10-206 nM), the most potent compounds 4d-4h (IC50 10-28 nM) bearing hydrophobic groups (Me, F, CF3 and Cl) in the terminal phenyl ring. A convincing rationalization was achieved for the highest potent compounds 4 as type II VEGFR-2 inhibitors, based on the simultaneous presence of: (1) the thioether linker and (2) the arylurea moiety in the meta position. For compounds 4, significant inhibition of Human Umbilical Vein Endothelial Cells (HUVECs) proliferation (BrdU assay), migration (wound-healing assay) and tube formation were observed at low concentrations. These compounds have also shown to increase apoptosis using the TUNEL assay. Immunostaining for total and phosphorylated (active) VEGFR-2 was performed by Western blotting. The phosphorylation of the receptor was significantly inhibited at 1.0 and 2.5 microM for the most promising compounds. Altogether, these findings point to an antiangiogenic effect in HUVECs.

Task clustering on ETL systems – A pattern-oriented approach

Usually, data warehousing populating processes are data-oriented workflows composed by dozens of granular tasks that are responsible for the integration of data coming from different data sources. Specific subset of these tasks can be grouped on a collection together with their relationships in order to form higher- level constructs. Increasing task granularity allows for the generalization of processes, simplifying their views and providing methods to carry out expertise to new applications. Well-proven practices can be used to describe general solutions that use basic skeletons configured and instantiated according to a set of specific integration requirements. Patterns can be applied to ETL processes aiming to simplify not only a possible conceptual representation but also to reduce the gap that often exists between two design perspectives. In this paper, we demonstrate the feasibility and effectiveness of an ETL pattern-based approach using task clustering, analyzing a real world ETL scenario through the definitions of two commonly used clusters of tasks: a data lookup cluster and a data conciliation and integration cluster.

Portuguese publication in the aim of regional science: a study of articles published in RPER from 2003 to 2015

This paper is a study of the full content of articles published by RPER, the Portuguese Review of Regional Studies, from the time it was launched in 2003 until the first quarter of 2015. RPER is a journal edited by the Portuguese section of the European Regional Science Association, which was established in the first half of the 1980s. The Association (APDR) and the journal are the result of contributions by researchers and technicians from different scientific fields, including mainly Economics, Geography, Sociology, Engineering and Architecture. The main focus of these contributions is the socio-economic life of concrete sites, and the way this life is conditioned by resources and capabilities, the historical and cultural heritage and institutions. Content analysis was undertaken to identify the main subjects chosen during the total period under analysis, the nature of the articles published (theoretical or empirical) and the main analytical framework used. The analysis also covers sub-periods to investigate major trends found in terms of subjects chosen and analytical methods, questioning the rationale behind them. The paper concludes with a few notes regarding the social echo the research received and an identification of the main limitations of the research. In the first part of the article, we conduct a summary review of the genesis and evolution of Regional Science at international level to serve as a basis for the empirical approach developed.

As imigrantes brasileiras no jornalismo impresso regional

O estudo sobre a representação das brasileiras nos media é revisto sob vários aspectos e nos diversos meios de comunicação. Alguns estudos aprofundam a imagem das imigrantes, enquanto outros se concentram nos meios (rádio, televisão e imprensa). Existe ainda uma linha de investigação que se centra nos estudos da recepção. Todavia, verificámos a escassez de um estudo específico sobre a representação deste grupo no jornalismo de proximidade. Esta comunicação tem por objectivo apresentar parte dos resultados sobre a representação dos imigrantes brasileiros nas notícias publicadas durante o ano de 2007 em dois jornais regionais (um português – Diário do Minho – e um italiano – L'Adige). A escolha de um jornal externo ao contexto português foi extremamente enriquecedora para identificar possíveis convergências no tratamento dos imigrantes brasileiros (homens e mulheres) em diferentes contextos sócioculturais. Além disso, tanto Portugal como Itália foram países de forte emigração, influenciando os processos migratórios de ambos. A investigação inicial mostrou uma acentuada assimetria de género, o que nos levou a aprofundar a análise sob este aspecto. Observámos que os jornais analisados, em relação ao tratamento informativo da imigrante brasileira, trabalham na mesma linha dos jornais de âmbito nacional e, mesmo que em escala inferior, continuam a representar estas mulheres com um baixo estatuto, associadas a temas e comportamentos socialmente conotados com a marginalidade. De salientar que as imigrantes brasileiras que têm visibilidade nas peças noticiosas dos dois jornais são geralmente conotadas com a prostituição, clandestinidade, crime e exploração.

All over the place localization system

The MAP-i Doctoral Programme in Informatics, of the Universities of Minho, Aveiro and Porto

Metaphorisms in programming

This paper introduces the metaphorism pattern of relational specification and addresses how specification following this pattern can be refined into recursive programs. Metaphorisms express input-output relationships which preserve relevant information while at the same time some intended optimization takes place. Text processing, sorting, representation changers, etc., are examples of metaphorisms. The kind of metaphorism refinement proposed in this paper is a strategy known as change of virtual data structure. It gives sufficient conditions for such implementations to be calculated using relation algebra and illustrates the strategy with the derivation of quicksort as example.

Índice Digital Regional 2014

O objetivo subjacente a toda a investigação que deu origem ao Índice Digital Regional (IDR), inserida num projeto de doutoramento, ia no sentido da “compreensão da realidade da Sociedade da Informação nas sete regiões NUTs II portuguesas, comparando-as e contrastando-as”. À semelhança do que acontece em grande parte dos indicadores de desenvolvimento, em que as assimetrias regionais são uma evidência verificada há várias décadas, importava perceber até que ponto o desenvolvimento da Sociedade da Informação em Portugal está a ser desencadeado sem ter ou não em atenção os valores da equidade, da coesão nacional e da solidariedade regional. Este artigo analisa os resultados do IDR recalculado com os dados estatísticos mais recentes.