Synthesis and Antiplasmodial Activity of 1,2,3-Triazole-Naphthoquinone Conjugates

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dc.contributor.authorSandra Oramas‐Royo
dc.contributor.authorPriscila López-Rojas
dc.contributor.authorÁngel Amesty
dc.contributor.authorDavid Gutiérrez
dc.contributor.authorNinoska Flores
dc.contributor.authorPatricia Martin‐Rodríguez
dc.contributor.authorLeandro Fernández‐Pérez
dc.contributor.authorAna Estévez‐Braun
dc.coverage.spatialBolivia
dc.date.accessioned2026-03-22T14:10:12Z
dc.date.available2026-03-22T14:10:12Z
dc.date.issued2019
dc.descriptionCitaciones: 38
dc.description.abstractA series of 34 1,2,3-triazole-naphthoquinone conjugates were synthesized via copper-catalyzed cycloaddition (CuAAC). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of <i>Plasmodium falciparum</i> and against three different tumor cell lines (SKBr-3, MCF-7, HEL). The most active antimalarial compounds showed a low antiproliferative activity. Simplified analogues were also obtained and some structure-activity relationships were outlined. The best activity was obtained by compounds <b>3s</b> and <b>3j,</b> having IC<sub>50</sub> of 0.8 and 1.2 μM, respectively. Molecular dockings were also carried on Plasmodium falciparum enzyme dihydroorotate dehydrogenase (<i>Pf</i>DHODH) in order to rationalize the results.
dc.identifier.doi10.3390/molecules24213917
dc.identifier.urihttps://doi.org/10.3390/molecules24213917
dc.identifier.urihttps://andeanlibrary.org/handle/123456789/44944
dc.language.isoen
dc.publisherMultidisciplinary Digital Publishing Institute
dc.relation.ispartofMolecules
dc.sourceUniversidad de La Laguna
dc.subjectDihydroorotate dehydrogenase
dc.subjectPlasmodium falciparum
dc.subjectNaphthoquinone
dc.subjectChemistry
dc.subjectTriazole
dc.subject1,2,3-Triazole
dc.subjectConjugate
dc.subjectCycloaddition
dc.subjectStereochemistry
dc.subjectCombinatorial chemistry
dc.titleSynthesis and Antiplasmodial Activity of 1,2,3-Triazole-Naphthoquinone Conjugates
dc.typearticle

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