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

Ullman, Brett R; Aja, Teresa; Deckwerth, Thomas L; Diaz, Jose-Luis; Herrmann, Julia; Kalish, Vincent J; Karanewsky, Donald S; Meduna, Steven P; Nalley, Kip; Robinson, Edward D; Roggo, Silvio P; Sayers, Robert O; Schmitz, Albert; Ternansky, Robert J; Tomaselli, Kevin J; Wu, Joe C

Ullman, Brett R; Aja, Teresa; Deckwerth, Thomas L; Diaz, Jose-Luis; Herrmann, Julia; Kalish, Vincent J; Karanewsky, Donald S; Meduna, Steven P; Nalley, Kip; Robinson, Edward D; Roggo, Silvio P; Sayers, Robert O; Schmitz, Albert; Ternansky, Robert J; Tomaselli, Kevin J; Wu, Joe C.

Afiliación

Ullman BR; Idun Pharmaceuticals, Inc., 9380 Judicial Drive, San Diego, CA 92121, USA. bullman@idun.com

Bioorg Med Chem Lett ; 13(20): 3623-6, 2003 Oct 20.

Article en En | MEDLINE | ID: mdl-14505683

RESUMEN

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.

Asunto(s)

Inhibidores de Caspasas; Inhibidores de Cisteína Proteinasa/química; Inhibidores de Cisteína Proteinasa/farmacología; Relación Estructura-Actividad

Buscar en Google

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Cisteína Proteinasa / Inhibidores de Caspasas Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2003 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

Buscar en Google

Añadir a Mi BVS

Imprimir

XML

PubMed Links