Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Bioorg Med Chem Lett
; 20(8): 2591-6, 2010 Apr 15.
Article
en En
| MEDLINE
| ID: mdl-20236824
ABSTRACT
A novel series of tricyclic gamma-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo profiles. More importantly, they have greatly reduced Notch related toxicity that was associated with previous gamma-secretase inhibitors.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Sulfonas
/
Receptores Notch
/
Secretasas de la Proteína Precursora del Amiloide
Límite:
Animals
Idioma:
En
Año:
2010
Tipo del documento:
Article