700372-68-5Relevant articles and documents
Proteasome inhibitors: Synthesis and activity of arecoline oxide tripeptide derivatives
Marastoni, Mauro,McDonald, John,Baldisserotto, Anna,Canella, Alessandro,Risi, Carmela De,Pollini, Gian Piero,Tomatis, Roberto
, p. 1965 - 1968 (2007/10/03)
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, compound 2 which contains 3-hydroxy-2-methylbenzoyl group at its N-terminal position, displayed the greatest inhibitory potency (IC50 1 μM). All derivatives showed favourable pharmacokinetic properties.