Journal
MOLECULES
Volume 24, Issue 21, Pages -Publisher
MDPI
DOI: 10.3390/molecules24213917
Keywords
malaria; Plasmodium falciparum; 1; 2; 3-triazole-naphthoquinones; copper-catalyzed cycloaddition; docking
Funding
- Spanish Ministerio de Economia y Competitividad (MINECO) [SAF 2015-65113-C2-1-R, SAF 2015-65113-C2-2-R]
- Agencia Canaria de Investigacion, Innovacion y Sociedad de la Informacion [2017010071]
- Ministerio de Ciencias, Innovacion y Universidades (MICINN) [RTI2018-094356-B-C21]
- European Regional Development Fund (FEDER)
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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 mu M, respectively. Molecular dockings were also carried on Plasmodium falciparum enzyme dihydroorotate dehydrogenase (PfDHODH) in order to rationalize the results.
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