Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.
Bioorg Med Chem Lett
; 21(13): 4036-40, 2011 Jul 01.
Article
en En
| MEDLINE
| ID: mdl-21621413
ABSTRACT
Starting from small molecule mTOR inhibitor Torin1, replacement of the piperazine ring with a phenyl ring resulted in a new series of mTOR inhibitors (as exemplified by 10) that showed superior potency and selectivity for mTOR, along with significantly improved mouse liver microsome stability and a longer in vivo half-life.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Microsomas Hepáticos
/
Descubrimiento de Drogas
/
Serina-Treonina Quinasas TOR
/
Naftiridinas
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos