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Inhibition of cancer cell growth and migration by dihydroxynaphthyl aryl ketones
Julio Benites,Jaime A. Valderrama,David Ríos,Rosalba Lagos,Octavio Monasterio,Pedro Buc Calderon,Pedro Buc Calderon 대한독성 유전단백체 학회 2016 Molecular & cellular toxicology Vol.12 No.3
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.