1,721,221 research outputs found

    Arylthioindoles, potent inhibitors of tubulin polymerization: structure-activity relationships and molecular modeling studies

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    Tubulin is a very important target for anticancer therapy. Recently, we reported several arylthioindoles with an excellent biological activity as inhibitors of tubulin polymerization and of some carcinoma cells.1,2 To investigate the structural basis of the SAR that emerged from the biological results, we carried out docking and molecular dynamics studies. Ethyl 5-methoxy-3-[(3,4,5-trimethoxyphenyl)thio]-1H-indole-2-carboxylate showed a very interesting binding mode into colchicine binding site of tubulin. References 1] De Martino, G.; La Regina, G.; Coluccia, A. et al. J. Med. Chem. 2004, 47, 6120-6123. 2] De Martino, G.; Michael C. Edler, M. C.; La Regina, G. et al. J. Med. Chem. 2006, 49, 947-954

    ABBANDONO E RIUSO IN ARCHITETTURA. L'USO TRANSITORIO COME PRATICA DI CONSERVAZIONE IN ULSTER

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    In Northern Ireland and especially in Belfast recent legislation has not prevented a series of building losses. These were abandoned and demolished in the name of a development idea based on building substitution. Already in the 60s of the twentieth century the prospect of economic development accelerated a series of unscrupulous operations, with unregulated growth in suburban areas, the construction of infrastructures that did not take into due account the urban proportions and a rapid decline of central areas; in addition to this the “Troubles” gave the coup de grace to physiological evolution of the city. Several associations and trusts were born to raise awareness and promote campaigns to rescue buildings at risk of demolition as a reaction to what was happening in the areas with higher density of historical buildings. Indeed, until not long ago the fine for modifying or even demolishing a listed building without permission were anything but a deterrent for such offence, but the action of these associations in many cases managed to avoid further losses for historical heritage. In addition to listed buildings, since 1993 the Heritage at Risk project has been set up, with the aim of providing support and advice to building owners who want to undertake appropriate maintenance plan and to support potential buyers interested in restoring a building at risk. A register to this effect (Built Heritage at Risk Northern Ireland or BHARNI) is managed by the Historic Buildings Unit of the Northern Ireland Environment Agency (NIEA) The main objectives of the BHARNI project are to register architecturally and historically significant buildings at risk and act as a catalyst for conservation and reuse of built heritage. In this perspective, it is also accepted the practice of carrying out a work phase that allows "meanwhile uses" or even "pop-up uses" to ease a process of re-appropriation even of large buildings for communities. at the same time "meanwhile use" guarantee at least maintenance, pending investments that allow a definitive restoration and a sustainable use
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