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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) |
| Appears in Collections: | Artículos |
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