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
em 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
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas Quinases
/
Pirimidinas
/
Triazinas
/
Morfolinas
/
Inibidores de Proteínas Quinases
/
Antineoplásicos
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article