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

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 ef...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-10, Vol.13 (20), p.3623-3626
Hauptverfasser:	ULLMAN, Brett R, AJA, Teresa, ROGGO, Silvio P, SAYERS, Robert O, SCHMITZ, Albert, TERNANSKY, Robert J, TOMASELLI, Kevin J, WU, Joe C, DECKWERTH, Thomas L, DIAZ, Jose-Luis, HERRMANN, Julia, KALISH, Vincent J, KARANEWSKY, Donald S, MEDUNA, Steven P, NALLEY, Kip, ROBINSON, Edward D
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Caspase Inhibitors Cysteine Proteinase Inhibitors - chemistry Cysteine Proteinase Inhibitors - pharmacology Medical sciences Pharmacology. Drug treatments Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00755-8