These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis and Antiplasmodial Activity of 1,2,3-Triazole-Naphthoquinone Conjugates.
    Author: Oramas-Royo S, López-Rojas P, Amesty Á, Gutiérrez D, Flores N, Martín-Rodríguez P, Fernández-Pérez L, Estévez-Braun A.
    Journal: Molecules; 2019 Oct 30; 24(21):. PubMed ID: 31671684.
    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.
    [Abstract] [Full Text] [Related] [New Search]