In vitro evaluation of triazenes: DNA cleavage, antibacterial activity and cytotoxicity against acute myeloid leukemia cells

Journal of the Brazilian Chemical Society

Vanessa O. Domingues²  Rosmari Hörner²  Luiz G. B. Reetz²  Fábio Kuhn²  Virgínia M. Coser¹  Jacqueline N. Rodrigues¹  Rita Bauchspiess¹  Waldir V. Pereira¹  Gustavo L. Paraginski¹  Aline Locatelli¹  Juliana De O. Fank¹  Vinícius F. Giglio¹  Manfredo Hörner¹ 

[1] ,Universidade Federal de Santa Maria Departamento de Análises Clínicas e Toxicológicas Santa Maria RS ,Brazil

关键词: triazenes;    DNA cleavage;    antibacterial activity;    cytotoxicit;   

DOI  :  10.1590/S0103-50532010001200009

来源: SciELO

【 摘 要 】

The asymmetric diazoamines 1-(2-chlorophenyl)-3-(4-carboxyphenyl)triazene (1), 1-(2-fluorophenyl)-3-(4-carboxyphenyl)triazene (2) and 1-(2-fluorophenyl)-3-(4-amidophenyl)triazene (3) were evaluated for their ability to cleave pUC18 and pBSKII plasmid DNA, antibacterial activity and in vitro cytotoxicity against acute myeloid leukemia cells and normal leukocytes using the bioassay of reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). The triazenes showed ability to cleave the two types of plasmid DNA: triazene 1 at pH 8.0 and 50 ºC; triazene 2 at pH 6.5 and 37 and 50 ºC; triazene 3 at pH 6.5 and 37 ºC. The compounds presented cytotoxic activity against myeloid leukemia cells. Compound 1 showed high activity against B. cereus (MIC = 32 mg mL-1). The observation of intermolecular hydrogen bonding in the solid state of compound 3, based on the structural analysis by X-ray crystallography, as well as the results of IR and UV-Vis spectroscopic analyses of compounds 1, 2 and 3 are discussed in the present work.

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