Unprecedented Inhibition of P-gp Activity by a Novel Ruthenium-Cyclopentadienyl Compound Bearing a Bipyridine-Biotin Ligand

Simple item page
UDC.coleccionInvestigaciónes_ES
UDC.departamentoQuímicaes_ES
UDC.endPage863es_ES
UDC.grupoInvGrupo de Investigación en Nanotoxicoloxía e Toxicoloxía Xenética (NANOTOXGEN)es_ES
UDC.institutoCentroCICA - Centro Interdisciplinar de Química e Bioloxíaes_ES
UDC.journalTitleEuropean Journal of Medicinal Chemistryes_ES
UDC.startPage853es_ES
UDC.volume163es_ES
dc.contributor.authorCôrte-Real, Leonor
dc.contributor.authorKaras, Brittany
dc.contributor.authorGírio, Patrícia
dc.contributor.authorMoreno, Alexis
dc.contributor.authorAvecilla, Fernando
dc.contributor.authorMarques, Fernanda
dc.contributor.authorBuckley, Brian T.
dc.contributor.authorCooper, Keith R.
dc.contributor.authorDoherty, Cathleen
dc.contributor.authorFalson, Pierre
dc.contributor.authorGarcia, Maria Helena
dc.contributor.authorValente, Andreia
dc.date.accessioned2025-01-13T16:26:22Z
dc.date.available2025-01-13T16:26:22Z
dc.date.issued2019-02-01
dc.descriptionThis is an accepted version of the published document.es_ES
dc.description.abstract[Abstract] Two new ruthenium complexes, [Ru(η5-Cp)(PPh3)(2,2’-bipy-4,4’-R)]+ with R = -CH2OH (Ru1) or dibiotin ester (Ru2) were synthesized and fully characterized. Both compounds were tested against two types of breast cancer cells (MCF7 and MDA-MB-231), showing better cytotoxicity than cisplatin in the same experimental conditions. Since multidrug resistance (MDR) is one of the main problems in cancer chemotherapy, we have assessed the potential of these compounds to overcome resistance to treatments. Ru2 showed exceptional selectivity as P-gp inhibitor, while Ru1 is possibly a substrate. In vivo studies in zebrafish showed that Ru2 is well tolerated up to 1.17 mg/L, presenting a LC50 of 5.73 mg/L at 5 days post fertilization.es_ES
dc.description.sponsorshipThis work was financed by the Portuguese Foundation for Science and Technology (Fundação para a Ciência e Tecnologia, FCT) within the scope of projects UID/QUI/00100/2013 and PTDC/QUI-QIN/28662/2017. Andreia Valente acknowledges the Investigator FCT2013 Initiative for the project IF/01302/2013 (acknowledging FCT, as well as POPH and FSE - European Social Fund). Leonor Côrte-Real thanks FCT for her Ph.D. Grant (SFRH/BD/100515/2014) and Fulbright Research Grant 2017/2018 with the support of FCT. Brittany Karas thanks NJAES-RutgersNJ01201, NIEHS Training Grant T32-ES 007148 and Brian Buckley, Cathleen Doherty NIEHS P30 ES005022. Keith R. Cooper thanks NJAES Project 01202 (W2045), NIH ES005022. Patrícia Gírio was funded by the Erasmus + Program and a fellowship received from the French National Research Agency, ANR-13-BSV5-0001-01 (to Dr. Pierre Falson)es_ES
dc.description.sponsorshipPortugal. Fundação para a Ciência e Tecnologia; UID/QUI/00100/2013es_ES
dc.description.sponsorshipPortugal. Fundação para a Ciência e Tecnologia; PTDC/QUI-QIN/28662/2017es_ES
dc.description.sponsorshipPortugal. Fundação para a Ciência e Tecnologia; IF/01302/2013es_ES
dc.description.sponsorshipPortugal. Fundação para a Ciência e Tecnologia; SFRH/BD/100515/2014es_ES
dc.description.sponsorshipNew Jersey Agricultural Experiment Station; NJ01201es_ES
dc.description.sponsorshipEstados Unidos. National Institute of Environmental Health Sciences; T32-ES 007148es_ES
dc.description.sponsorshipEstados Unidos. National Institute of Environmental Health Sciences; P30 ES005022es_ES
dc.description.sponsorshipNew Jersey Agricultural Experiment Station; 01202 (W2045)es_ES
dc.description.sponsorshipEstados Unidos. National Institutes of Health; ES005022es_ES
dc.description.sponsorshipFrancia. Agence nationale de la recherche; ANR-13-BSV5-0001-01es_ES
dc.identifier.citationLeonor Côrte-Real, Brittany Karas, Patrícia Gírio, Alexis Moreno, Fernando Avecilla, Fernanda Marques, Brian T. Buckley, Keith R. Cooper, Cathleen Doherty, Pierre Falson, M. Helena Garcia, Andreia Valente, Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand, European Journal of Medicinal Chemistry, Volume 163, 2019, Pages 853-863, ISSN 0223-5234, https://doi.org/10.1016/j.ejmech.2018.12.022es_ES
dc.identifier.doi10.1016/j.ejmech.2018.12.022
dc.identifier.issn0223-5234
dc.identifier.urihttp://hdl.handle.net/2183/40681
dc.language.isoenges_ES
dc.publisherElsevieres_ES
dc.relation.urihttps://doi.org/10.1016/j.ejmech.2018.12.022es_ES
dc.rightsAtribución-NoComercial-SinDerivadas 4.0 Internacionales_ES
dc.rights.accessRightsopen accesses_ES
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectRuthenium organometallic compoundses_ES
dc.subjectAnticancer agentses_ES
dc.subjectP-gp inhibitores_ES
dc.subjectMultidrug resistancees_ES
dc.titleUnprecedented Inhibition of P-gp Activity by a Novel Ruthenium-Cyclopentadienyl Compound Bearing a Bipyridine-Biotin Ligandes_ES
dc.typejournal articlees_ES
dspace.entity.typePublication
relation.isAuthorOfPublicationf1e8634f-151e-4b2e-9fe9-10aabc85c38e
relation.isAuthorOfPublication.latestForDiscoveryf1e8634f-151e-4b2e-9fe9-10aabc85c38e

Files

Original bundle

Now showing 1 - 1 of 1
Thumbnail Image
Name:
Avecilla_Fernando_2019_Unprecedented_inhibition_P-gp_activity.pdf
Size:
2.18 MB
Format:
Adobe Portable Document Format
Description:
Download

Collections

Investigación (FCIE)