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- W2058492198 abstract "Abstract We demonstrate that the cytotoxicity of dansylated polytheonamide mimic ( 2 ) is controlled by chemical modification of its N-terminal structure. Dansylated polytheonamide mimic ( 2 ) is an ion channel peptide which displays potent cytotoxicity against P388 mouse leukemia cells (IC 50 = 12 nM). To modulate its cytotoxicity, three analogues of 2 , possessing distinct N-terminal structures with different hydrophobicities, were synthesized and their cytotoxicities were evaluated. This focused structure–activity relationship study unveiled that the cytotoxicity of 2 is enhanced 10-fold by simply changing its N-terminal 5,5-dimethyl-2-oxohexanamide to the more hydrophobic palmitamide. The data obtained here provide new understanding for the functional control of the artificial ion channel peptide 2 ." @default.
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- W2058492198 date "2014-01-01" @default.
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- W2058492198 title "Control of the cytotoxicity of dansylated polytheonamide mimic, an artificial peptide ion channel, by modification of the N-terminal structure" @default.
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- W2058492198 doi "https://doi.org/10.1016/j.tetlet.2013.12.007" @default.
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