Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
Bioorg Med Chem Lett
; 19(20): 5898-901, 2009 Oct 15.
Article
en En
| MEDLINE
| ID: mdl-19733066
ABSTRACT
A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series based on a tri-substituted triazine scaffold has led to the discovery of potent and selective inhibitors of mTOR.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Proteínas Quinasas
/
Pirimidinas
/
Triazinas
/
Morfolinas
/
Inhibidores de Proteínas Quinasas
/
Antineoplásicos
Tipo de estudio:
Diagnostic_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2009
Tipo del documento:
Article
País de afiliación:
Reino Unido