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Cytotoxic and DNA-topoisomerase effects of lapachol amine derivatives and interactions with DNA BJMBR
Esteves-Souza,A.; Figueiredo,D.V.; Esteves,A.; Câmara,C.A.; Vargas,M.D.; Pinto,A.C.; Echevarria,A..
The cytotoxic activity of amino (3a-e), aza-1-antraquinone (4a-e) lapachol derivatives against Ehrlich carcinoma and human K562 leukemia cells was investigated. Cell viability was determined using MTT assay, after 48 (Ehrlich) or 96 h (K562) of culture, and vincristine (for K562 leukemia) and quercetin (for Ehrlich carcinoma) were used as positive controls. The results showed dose-dependent growth-inhibiting activities and that the amino derivatives were active against the assayed cells, whereas the 4a-e derivatives were not. The allylamine derivative 3a was the most active against Ehrlich carcinoma, with IC50 = 16.94 ± 1.25 µM, and against K562 leukemia, with IC50 = 14.11 ± 1.39 µM. The analogous lawsone derivative, 5a, was also active against Ehrlich...
Tipo: Info:eu-repo/semantics/other Palavras-chave: Lapachol; Amino-lapachol derivatives; Cytotoxicity; DNA-topoisomerase; DNA-interactions.
Ano: 2007 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2007001000013
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