1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Bioorg Med Chem
; 22(8): 2416-26, 2014 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-24656804
ABSTRACT
A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50=1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tiazoles
/
Morfolinas
/
Benzotiazoles
/
Caspasa 3
/
Inhibidores de Caspasas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2014
Tipo del documento:
Article
País de afiliación:
China