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http://hdl.handle.net/10261/178024
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Campo DC | Valor | Lengua/Idioma |
---|---|---|
dc.contributor.author | Staderini, Matteo | es_ES |
dc.contributor.author | Piquero, Marta | es_ES |
dc.contributor.author | Abengozar, M. A. | es_ES |
dc.contributor.author | Nácher-Vázquez, Montserrat | es_ES |
dc.contributor.author | Romanelli, Giulia | es_ES |
dc.contributor.author | López-Alvarado, Pilar | es_ES |
dc.contributor.author | Rivas, Luis | es_ES |
dc.contributor.author | Bolognesi, Maria Laura | es_ES |
dc.contributor.author | Menéndez, J. Carlos | es_ES |
dc.date.accessioned | 2019-03-15T13:23:31Z | - |
dc.date.available | 2019-03-15T13:23:31Z | - |
dc.date.issued | 2019-03-14 | - |
dc.identifier.citation | European Journal of Medicinal Chemistry 171: 38-53 (2019) | es_ES |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | http://hdl.handle.net/10261/178024 | - |
dc.description | 58 p.-6 fig.-1 tab.-5 schem.-1 graph.abst | es_ES |
dc.description.abstract | A new class of quinoline derivatives, bearing amino chains at C-4 and a styryl group at C-2, were tested on Leishmania donovani promastigotes and axenic and intracellular Leishmania pifanoi amastigotes. The introduction of the C-4 substituent improves the activity, which is due to interference with the mitochondrial activity of the parasite and its concomitant bioenergetic collapse by ATP exhaustion. Some compounds show a promising antileishmanial profile, with low micromolar or submicromolar activity on promastigote and amastigote forms and a good selectivity index. | es_ES |
dc.description.sponsorship | This research was supported by the following grants; (a) MLB: MIUR, PRIN 201274BNKN_003; (b) JCM: Universidad Complutense (GR3/14) and MINECO (CTQ2015-68380-R); (c) LR: RD16/0027/0010, CSIC PIE-201020E054 and MINECO SAF2015-65740-R. A predoctoral contracts to MS from Universidad Complutense and a FPI contract to MP from MINECO (BES-2016–076410P) are also gratefully acknowledged. | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | Elsevier | es_ES |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/CTQ2015-68380-R | es_ES |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/SAF2015-65740-R | es_ES |
dc.relation.isversionof | Postprint | es_ES |
dc.rights | openAccess | en_EN |
dc.subject | Leishmanicidal compounds | es_ES |
dc.subject | 4-Aminoquinolines | es_ES |
dc.subject | 2-Styrylquinolines | es_ES |
dc.subject | Mitochondrial metabolism | es_ES |
dc.title | Structure-activity relationships and mechanistic studies of novel mitochondria-targeted, leishmanicidal derivatives of the 4-aminostyrylquinoline scaffold | es_ES |
dc.type | artículo | es_ES |
dc.identifier.doi | 10.1016/j.ejmech.2019.03.007 | - |
dc.description.peerreviewed | Peer reviewed | es_ES |
dc.relation.publisherversion | https://doi.org/10.1016/j.ejmech.2019.03.007 | es_ES |
dc.identifier.e-issn | 1768-3254 | - |
dc.embargo.terms | 2020-03-14 | es_ES |
dc.contributor.funder | Ministero dell'Istruzione, dell'Università e della Ricerca | es_ES |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | es_ES |
dc.contributor.funder | Universidad Complutense de Madrid | es_ES |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | es_ES |
dc.contributor.funder | Instituto de Salud Carlos III | es_ES |
dc.relation.csic | Sí | es_ES |
oprm.item.hasRevision | no ko 0 false | * |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100002911 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100004587 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003407 | es_ES |
dc.contributor.orcid | Abengozar, M. A. [0000-0002-2432-3512] | es_ES |
dc.contributor.orcid | Nácher-Vázquez, Montserrat [0000-0001-8355-8373] | es_ES |
dc.contributor.orcid | López-Alvarado, Pilar [0000-0002-5773-2339] | es_ES |
dc.contributor.orcid | Rivas, Luis, [0000-0002-2958-3233] | es_ES |
dc.contributor.orcid | Bolognesi, Maria Laura [0000-0002-1289-5361] | es_ES |
dc.contributor.orcid | Menéndez, J. Carlos [0000-0002-0560-8416] | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.fulltext | With Fulltext | - |
item.languageiso639-1 | en | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.openairetype | artículo | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | open | - |
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Fichero | Descripción | Tamaño | Formato | |
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J. Med. Chem._Staderini_2019.pdf | Postprint | 2,79 MB | Adobe PDF | Visualizar/Abrir |
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