We describe the synthesis and biological activities of a series of methyl 3,4-epoxypiperidine-3-carboxylate tripeptide derivatives that inhibit the chymotryptic and tryptic active sites of the 20S proteasome. Of the series, the compound containing 3-hydroxy-2-methylbenzoyl group at its N-terminal position, displayed the greatest inhibitory potency. All derivatives showed favourable pharmacokinetic properties.
Proteasome inhibitors: synthesis and activity of arecoline oxide tripeptide derivatives
MARASTONI, Mauro;BALDISSEROTTO, Anna;CANELLA, Alessandro;DE RISI, Carmela;POLLINI, Gian Piero;TOMATIS, Roberto
2004
Abstract
We describe the synthesis and biological activities of a series of methyl 3,4-epoxypiperidine-3-carboxylate tripeptide derivatives that inhibit the chymotryptic and tryptic active sites of the 20S proteasome. Of the series, the compound containing 3-hydroxy-2-methylbenzoyl group at its N-terminal position, displayed the greatest inhibitory potency. All derivatives showed favourable pharmacokinetic properties.File in questo prodotto:
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