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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.10.047
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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2006.10.047
Date Deposited:	14 Dec 2009 13:57
Last Modified:	31 Jan 2013 01:13
URI:	https://oak.novartis.com/id/eprint/572