Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Imbach, Patricia, Lang, Marc, Garcia-Echeverria, Carlos, Guagnano, Vito, Noorani, Maria, Roesel, Johannes, Bitsch, Francis, Rihs, Grety and Furet, Pascal (2007) Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorganic & Medicinal Chemistry Letters, 17 (2). pp. 358-362. ISSN 0960-894X
Abstract
A series of beta-lactam derivatives has been designed and synthesized to inhibit the chymotrypsin-like activity of the human 20S proteasome. The most potent compounds of this new structural class of beta-subunit selective 20S proteasome inhibitors exhibit IC50 values in the low-nanomolar range and show good selectivity over the trypsin-like and post-glutamyl-peptide hydrolytic activities of the enzyme.
Item Type: | Article |
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Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
Keywords: | Proteasome inhibitors; β-Lactams; Covalent inhibitors; Antiproliferative agents |
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Date Deposited: | 14 Dec 2009 13:57 |
Last Modified: | 31 Jan 2013 01:13 |
URI: | https://oak.novartis.com/id/eprint/572 |