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Two series of dioscin derivatives (4a–o and 5a–o) with selected modifications at the 6′ and 4‴ positions of the chacotriosyl residue, respectively, were synthesized. All the 6′-N-acyl-dioscin derivatives did not show considerable inhibitory activities at 10μM, while most of the 4‴-O-(2-N-acyl)ethyl-dioscin derivatives behaved as potent as dioscin, against the growth of tumor cells.
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