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
em 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
Base de dados:
MEDLINE
Assunto principal:
Sulfonas
/
Receptores Notch
/
Secretases da Proteína Precursora do Amiloide
Limite:
Animals
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article