Novel GSK-3 inhibitors with improved cellular activity.
Bioorg Med Chem Lett
; 14(9): 2127-30, 2004 May 03.
Article
em En
| MEDLINE
| ID: mdl-15080993
ABSTRACT
A novel series of [1-(1H-benzimidazol-7-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl] arylhydrazones was synthesized and shown to potently inhibit glycogen synthase kinase-3 (GSK-3). In light of detailed structure-activity relationships and structural knowledge of the GSK-3 binding pocket, a benzimidazole substituent was incorporated onto the pyrazolopyrimidine core resulting in improved potency over previous analogs. More importantly, these derivatives show low nanomolar efficacy for stimulating glycogen synthesis in vitro and therefore may be useful in the treatment of type 2 diabetes mellitus.
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Base de dados:
MEDLINE
Assunto principal:
Quinase 3 da Glicogênio Sintase
/
Inibidores Enzimáticos
/
Hidrazonas
Limite:
Animals
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article