Discovery and SAR of spirochromane Akt inhibitors.
Bioorg Med Chem Lett
; 21(8): 2410-4, 2011 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-21392984
ABSTRACT
A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteínas Quinases
/
Proteínas Proto-Oncogênicas c-akt
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article