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Título: | Linear and branched alkyl-esters and amides of gallic acid and other (mono-, di- and tri-) hydroxy benzoyl derivatives as promising anti-HCV inhibitors |
Autor: | Rivero-Buceta, Eva CSIC ORCID; Carrero, Paloma CSIC; Doyagüez, Elisa G. CSIC; Madrona, Andrés CSIC ORCID; Quesada, Ernesto CSIC ORCID ; Camarasa Rius, María José CSIC ORCID; Peréz-Pérez, María-Jesús CSIC ORCID ; Leyssen, Pieter; Paeshuyse, Jan; Balzarini, Jan; Neyts, Johan; San-Félix, Ana CSIC ORCID | Palabras clave: | Polyphenols HIV AIDS Antiviral agents HCV |
Fecha de publicación: | 2015 | Editor: | Elsevier | Citación: | European Journal of Medicinal Chemistry 92: 656-671 (2015) | Resumen: | Linear and branched compounds that contain two, three or five units of galloyl (3,4,5-trihydroxybenzoyl) or its isomer 2,3,4-trihydroxybenzoyl, as well as other mono- or dihydroxybenzoyl moieties have been synthesized. These molecules have been evaluated for their in vitro inhibitory effects against a wide panel of viruses showing preferential activity against HIV and HCV. Our structure-activity relationship studies demonstrated that the 2,3,4-trihydroxybenzoyl moiety provides better antiviral activities than the galloyl (3,4,5-trihydroxybenzoyl) moiety that is present in natural green tea catechins. This observation can be of interest for the further rational exploration of compounds with anti-HCV/HIV properties. The most notable finding with respect to HIV is that the tripodal compounds 43 and 45, with three 2,3,4-trihydroxybenzoyl moieties, showed higher activities than linear compounds with only one or two. With respect to HCV, the linear compounds, 52 and 41, containing a 12 polymethylene chain and two 2,3 di- or 2,3,4 tri-hydroxybenzoyl groups respectively at the ends of the molecule showed good antiviral efficiency. Furthermore, the anti-HCV activity of both compounds was observed at concentrations well below the cytotoxicity threshold. A representative member of these compounds, 41, showed that the anti-HCV activity was largely independent of the genetic make-up of the HCV subgenomic replicon and cell lines used. | Versión del editor: | http://dx.doi.org/10.1016/j.ejmech.2015.01.033 | URI: | http://hdl.handle.net/10261/110851 | DOI: | 10.1016/j.ejmech.2015.01.033 | Identificadores: | doi: 10.1016/j.ejmech.2015.01.033 issn: 0223-5234 e-issn: 1768-3254 |
Aparece en las colecciones: | (CENQUIOR) Artículos (IQM) Artículos |
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ASF2Manuscript EJMECH-D-14-01438R2.pdf | 1,03 MB | Adobe PDF | Visualizar/Abrir |
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