Synthesis and antiplasmodial activity of 1,2,3-triazole-naphthoquinone conjugates

Sandra Oramas-Royo, Priscila López-Rojas, Ángel Amesty, David Gutiérrez, Ninoska Flores, Patricia Martín-Rodríguez, Leandro Fernández-Pérez, Ana Estévez-Braun

Resultado de la investigación: Contribución a una revistaArtículorevisión exhaustiva

10 Citas (Scopus)

Resumen

A 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 Plasmodium falciparum 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 3s and 3j, having IC50 of 0.8 and 1.2 μM, respectively. Molecular dockings were also carried on Plasmodium falciparum enzyme dihydroorotate dehydrogenase (PfDHODH) in order to rationalize the results.

Idioma originalInglés
Número de artículo3917
PublicaciónMolecules
Volumen24
N.º21
DOI
EstadoPublicada - 2019

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© 2019 by the authors.

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