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Synthesis of chalcones derived from 1-naphthylacetophenone and evaluation of their cytotoxic and apoptotic effects in acute leukemia cell lines

2021; Elsevier BV; Volume: 116; Linguagem: Inglês

10.1016/j.bioorg.2021.105315

1090-2120

Amanda Virtuoso Jacques, Natália Marcéli Stefanes, Laura Otto Walter, Daiane Perondi, Fernanda da Luz Efe, Luiz Felipe Schmitz de Souza, Larissa Sens, Stephanie Milis Syracuse, Ana Carolina Rabello de Moraes, Aldo Sena de Oliveira, C. Martins, Luma G. Magalhães, Adriano D. Andricopulo, Lisandra de Oliveira Silva, Ricardo José Nunes, Maria Cláudia Santos‐Silva,

Synthesis and Biological Evaluation

Chalcones and their derivatives have been described as promising compounds with antiproliferative activity against leukemic cells. This study aimed to investigate the cytotoxic effect of three synthetic chalcones derived from 1-naphthylacetophenone (F07, F09, and F10) in acute leukemia cell lines (K562 and Jurkat) and examine the mechanisms of cell death induced by these compounds. The three compounds were cytotoxic to K562 and Jurkat cells, with IC50 values ranging from 1.03 to 31.66 µM. Chalcones induced intrinsic and extrinsic apoptosis, resulting in activation of caspase-3 and DNA fragmentation. F07, F09, and F10 were not cytotoxic to human peripheral blood mononuclear cells, did not produce any significant hemolytic activity, and did not affect platelet aggregation after ADP stimulation. These results, combined with calculations of molecular properties, suggest that chalcones F07, F09, and F10 are promising molecules for the development of novel antileukemic drugs.