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dc.contributor.author | Flores, Aida | - |
dc.contributor.author | Camarasa Rius, María José | - |
dc.contributor.author | Peréz-Pérez, María-Jesús | - |
dc.contributor.author | San-Félix, Ana | - |
dc.contributor.author | Balzarini, Jan | - |
dc.contributor.author | Quesada, Ernesto | - |
dc.date.issued | 2014 | - |
dc.identifier | doi: 10.1039/c4ob00445k | - |
dc.identifier | issn: 1477-0520 | - |
dc.identifier | e-issn: 1477-0539 | - |
dc.identifier.citation | Organic and Biomolecular Chemistry 12: 5278-5294 (2014) | - |
dc.identifier.uri | http://hdl.handle.net/10261/100972 | - |
dc.description.abstract | The synthesis and the assessment of the anti-HIV activity of a set of molecules inspired by the multivalent structures of some naturally-occurring polyphenols (tannins) are reported. Different multibranched scaffolds have been derived from pentaerythritol as the central core which distribute spatially synthetic polyphenolic subunits based on 1-substituted 2,3,4-trihydroxyphenyl moieties. A tetrapodal compound (13b) bearing four N-(2,3,4-trihydroxyphenyl) amide groups, exhibits remarkable selective activity against HIV-1 with EC 50 values in the micromolar scale, in the same range as those reported for the most representative anti-HIV tannins. Preliminary SAR studies emphasize the importance of the 1-substituted 2,3,4-trihydroxyphenyl moiety, the presence of an amide as the linker and the multivalent architecture of these molecules, since the anti-HIV activity increases with the number of polyphenolic moieties. The data support the interest in synthetic polyphenols and represent a promising starting point for further design and development of selective HIV-1 inhibitors. | - |
dc.description.sponsorship | This work has been supported by the Spanish MICINN/ MINECO (projects SAF2009-13914-C02-01 and SAF2012-39760- C02-01), Comunidad de Madrid (BIPEDD-2 project CM-S2010/ BMD-2457) and the KU Leuven (GOA no. 10/014; EF 05/15; PF 10/018). Dr A. Flores acknowledges financial support from a contract JAE-Doc (Programa Junta para la Ampliación de Estu- dios) co-funded by CSIC and UE (FSE, Fondo Social Europeo). Sonsoles Velázquez is acknowledged for critical reading and valuable comments on this article and Leen Ingels for dedi- cated technical assistance with the antiviral assays | - |
dc.description.sponsorship | We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI) | - |
dc.publisher | Royal Society of Chemistry (UK) | - |
dc.rights | openAccess | - |
dc.title | Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1 | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1039/c4ob00445k | - |
dc.relation.publisherversion | http://dx.doi.org/10.1039/c4ob00445k | - |
dc.date.updated | 2014-08-21T10:33:09Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.contributor.funder | Ministerio de Ciencia e Innovación (España) | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.contributor.funder | Comunidad de Madrid | - |
dc.contributor.funder | University of Leuven | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100004837 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/100012818 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.cerifentitytype | Publications | - |
item.grantfulltext | open | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
item.openairetype | artículo | - |
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Org. Biomol. Chem., 2014.pdf | 4,24 MB | Adobe PDF | Visualizar/Abrir |
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