Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy.
Bioorg Med Chem Lett
; 22(7): 2411-4, 2012 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-22406151
ABSTRACT
The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The elaboration of a lead pyrrole derivative to a bicyclic dihydroindolone core provided compounds with high potency and good drug-like pharmaceutical properties. Further scaffold modification afforded a series of dihydroindolizinone inhibitors, including an orally available advanced preclinical MEK inhibitor with potent in vivo antitumor efficacy.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
MAP Quinase Quinase Quinases
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Inibidores de Proteínas Quinases
/
Indolizinas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2012
Tipo de documento:
Article