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KMID : 1034820160120030237
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Molecular & Cellular Toxicology
2016 Volume.12 No. 3 p.237 ~ p.242
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Inhibition of cancer cell growth and migration by dihydroxynaphthyl aryl ketones
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Benites Julio
Valderrama Jaime A.
Rios David
Lagos Rosalba
Monasterio Octavio
Calderon Pedro Buc
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Abstract
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Dihydroxynaphthyl aryl ketones 1-5 exhibit activity as tubulin polymerization inhibitors by targeting the colchicine binding site of microtubules making them potential anticancer drugs. Therefore, analogues 1-5 have been evaluated for their cytotoxic activity against the cancer cell lines DU-145 (prostate), T24 (bladder) and MCF-7 (breast). Notable differences in biological activity were observed for compounds 1-5, most likely related to the nature of the aryl substituent bonded to the carbonyl group. Among the tested compounds, only compound 5 showed selectivity for cancer cells over healthy, non-transformed cells. T24 cancer cells treated with compound 5 presented a concentration-dependent decrease in cell proliferation and a loss of migration ability. The cytotoxicity of compounds 1-5 on the selected cell-based assays is discussed in terms of it lipophilicity and polarizability parameters.
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KEYWORD
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Cytotoxicity, Dihydroxynaphthyl aryl ketones, Cell migration, Cell proliferation, Lipophilicity
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