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  • Title: Proteasome inhibitors; synthesis and activity of arecoline oxide tripeptide derivatives.
    Author: Marastoni M, McDonald J, Baldisserotto A, Canella A, De Risi C, Pollini GP, Tomatis R.
    Journal: Bioorg Med Chem Lett; 2004 Apr 19; 14(8):1965-8. PubMed ID: 15050638.
    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, compound 2 which contains 3-hydroxy-2-methylbenzoyl group at its N-terminal position, displayed the greatest inhibitory potency (IC(50) <1 microM). All derivatives showed favourable pharmacokinetic properties.
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