Produção Nacional
Revisado por pares
Synthesis and cytotoxicity evaluation of thiosemicarbazones and their thiazole derivatives
2016; UNIVERSIDADE DE SÃO PAULO; Volume: 52; Issue: 2 Linguagem: Inglês
10.1590/s1984-82502016000200008
ISSN2175-9790
AutoresSaulo Fehelberg Pinto Braga, Nayara Cristina Fonseca, Jonas Pereira Ramos, Elaine M. Souza–Fagundes, Renata Barbosa de Oliveira,
Tópico(s)Metal complexes synthesis and properties
ResumoABSTRACT The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells) cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazide (yield 71-96%), which were subjected to a cyclization with α-bromoacetophenone to yield the required thiazole heterocycles (yield 63-100%). All the synthesized compounds were screened at 50 µM concentration against three cell lines representing HL60 (promyelocytic leukemia), Jurkat (acute lymphoblastic leukemia), and MCF-7 (breast cancer). The pro-apoptotic effect was measured by flow cytometry as the percentage of cells with hypodiploid DNA. Results: Three thiazole compounds showed activity against at least one tumor cell line (IC50 = 43-76 µM) and low cytotoxicity against Vero cells (IC50 > 100 M). The most active compound of this series induced 91% and 51% DNA fragmentation in HL60 and MCF-7 cell lines, respectively, suggesting that this compound triggered apoptosis in these cells. Conclusion: Among the synthesized compounds, one in particular was found to exert antiproliferative and pro-apoptotic activity on tumor cells and can be considered promising as a lead molecule for the design of new analogues with improved activity.
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