Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/70087
Title: Synthesis and antiplasmodial activity of 1,2,3-triazole-naphthoquinone conjugates
Authors: Oramas-Royo, Sandra
López-Rojas, Priscila
Amesty, Ángel
Gutiérrez, David
Flores, Ninoska
Martín-Rodríguez, Patricia 
Fernández-Pérez, Leandro 
Estévez-Braun, Ana
UNESCO Clasification: 32 Ciencias médicas
Keywords: 1,2,3-Triazole-Naphthoquinones
Copper-Catalyzed Cycloaddition
Docking
Malaria
Plasmodium Falciparum
Issue Date: 2019
Project: Desarrollo Preclínico de Nuevas Estructuras Bioactivas Moduladoras de Las Actividades Oncogénicas de Stat3/5 O de Los Receptores de Estrógenos 
Journal: Molecules 
Abstract: 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.
URI: http://hdl.handle.net/10553/70087
ISSN: 1420-3049
DOI: 10.3390/molecules24213917
Source: Molecules [1420-3049], v. 24 (21)
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