1.
Bioorg Med Chem Lett
; 15(15): 3632-6, 2005 Aug 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15964758
RESUMO
Various heterocyclic hetero-methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A study of their structure-activity relationship (SAR) related to caspase-1, -3, -6, and -8 is reported. Their efficacy in a cellular model of cell death is also discussed. Potent broad-spectrum caspase inhibitors have been identified.
Assuntos
Inibidores de Caspase , Morte Celular/efeitos dos fármacos , Inibidores de Cisteína Proteinase/farmacologia , Compostos Heterocíclicos/farmacologia , Cetonas/farmacologia , Animais , Ácido Aspártico/química , Células Cultivadas , Compostos Heterocíclicos/síntese química , Cetonas/síntese química , Camundongos , Modelos Biológicos , Naftóis/química , Relação Estrutura-Atividade , Valina/química
2.
Bioorg Med Chem Lett
; 13(20): 3623-6, 2003 Oct 20.
Artigo
em Inglês
| MEDLINE
| ID: mdl-14505683
RESUMO
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.