Made available in DSpace on 2022-04-29T02:17:15Z (GMT). No. of bitstreams: 0 Previous issue date: 2011-12-29; Background: Animal venoms are complex mixtures of proteins and non proteins components with several biological activities. Snake venoms represent an essentially unexplored source of bioactive compounds that may cure disease conditions which do not respond to currently available therapies. These venoms p...
In recent decades, the incidence of candidemia in tertiary hospitals worldwide has substantially increased. These infections are a major cause of morbidity and mortality; in addition, they prolong hospital stays and raise the costs associated with treatment. Studies have reported a significant increase in infections by non-albicans Candida species, especially C. tropicalis. The number of antifungal drugs on the...
A series of thirty-two isoniazid derivatives have been evaluated for their activity against four human cancer cell lines with potent cytotoxicity (IC50 ranging from 0.61 to 3.36 μg/mL). The structure-activity relationship (SAR) analysis indicated the number, the positions, and the types of substituents attached to the aromatic ring as being critical factors for the biological activity. Briefly, we observed that...
A series of fifty-four commercial aldehydes have been synthesized and evaluated for their activity against peripheral blood mononuclear cells (PBMC) and four human cancer cell lines, exhibiting potent citotoxicity (IC50 ranging from 0.36 to 4.75 μg mL-1). The structureactivity relationship (SAR) analysis indicated that the number, the positions and the type of substituents attached into the aromatic and heteroa...
A series of 23 racemic mefloquine–oxazolidine derivatives, 4-[3-(aryl)hexahydro[1,3]oxazolo[3,4-a]pyridin- 1-yl]-2,8-bis(trifluoromethyl)quinolines, derived from (R*, S*)-(±)-mefloquine and arenealdehydes, have been evaluated for their activity against four cancer cell lines (HCT-8, OVCAR-8, HL-60, and SF-295). Good cytotoxicities have been determined with IC50 values ranging from 0.59 to 4.79 lg/mL. In general...
The current study describes that nor-β-lapachone and its arylamino derivatives, iodinated and methylated naphthoquinones and nor-β-lapachone-based 1,2,3-triazoles exhibited pronounced cytotoxic effects against four human leukemia cell lines (HL-60, K562, Molt-4 and Jurkat). Nor-β- lapachones arylamino substituted with potent activity were identified, revealing themselves as potential prototypes against tumor ce...
b-lapachone, a DNA repair inhibitor, has been recognized as important prototype with activity against cancer cells devoided of cytotoxicity in non-tumor cells. NQO1 is a reductive enzyme that is important for the activation of many bioreductive quinones. Thus, differential levels of NQO1 in tissues, including tumors, can provide a target for an enzyme-directed approach to cancer therapy. Herein, we aimed to eva...
Essential oil (EO) of Alpinia zerumbet leaves, at non-toxic concentrations (50–300 l g/mL), did not induce genotoxicity in human leukocytes. However, at the highest concentration (500 l g/mL) tested caused a reduction in cell proliferation and viability, and an increase in DNA damage. Moreover, in vivo experi- ments showed that EO (400 mg/kg) did not exert mutagenicity on peripheral blood cells and bone mar- ro...