Structure–Activity relationships within a series of caspase inhibitors: effect of leaving group modifications

Autor:	Edward D. Robinson, Silvio Roggo, Joe C. Wu, Robert J. Ternansky, Jose-Luis Diaz, Teresa Aja, Kevin J. Tomaselli, Steven P. Meduna, Vincent J. Kalish, Donald S. Karanewsky, Robert O. Sayers, Albert Schmitz, Brett R. Ullman, Julia Herrmann, Kip Nalley, Thomas L. Deckwerth
Rok vydání:	2003
Předmět:	chemistry.chemical_classification Programmed cell death biology Chemistry Organic Chemistry Clinical Biochemistry Leaving group Pharmaceutical Science Inflammation Cysteine Proteinase Inhibitors Caspase Inhibitors Biochemistry In vitro Structure-Activity Relationship Enzyme Enzyme inhibitor Drug Discovery biology.protein medicine Molecular Medicine Structure–activity relationship medicine.symptom Molecular Biology Caspase
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:3623-3626
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::681ec055be84e31c81b8947185e1442d https://doi.org/10.1016/s0960-894x(03)00755-8 Zobrazit plný text záznamu Full Text from ScienceDirect