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Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications

Ullman, Brett R and Aja, Teresa and Deckwerth, Thomas L and Diaz, Jose-Luis and Herrmann, Julia and Kalish, Vincent J and Karanewsky, Donald S and Meduna, Steven P and Nalley, Kip and Robinson, Edward D and Roggo, Silvio and Sayers, Robert O and Schmitz, Albert and Ternansky, Robert J and Tomaselli, Kevin J and Wu, Joe C (2003) Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications. Bioorganic & Medicinal Chemistry Letters, 13 (20). pp. 3623-3626. ISSN 0960-894X

Abstract

Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum caspase inhibitors have been identified. Their efficacy in cellular models of cell death and inflammation are also discussed.

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
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Date Deposited: 29 Apr 2010 23:45
Last Modified: 01 Feb 2013 00:49
URI: https://oak.novartis.com/id/eprint/2861

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