Indole RSK inhibitors. Part 1: discovery and initial SAR.
Bioorg Med Chem Lett
; 22(1): 733-7, 2012 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-22100312
ABSTRACT
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were identified through high throughput screening. An RSK crystal structure and exploratory SAR were used to define the series pharmacophore. Compounds with good cell potency, such as compounds 43, 44, and 55 were identified, and form the basis for subsequent kinase selectivity optimization.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Azepinas
/
Proteínas Quinases S6 Ribossômicas 90-kDa
/
Inibidores Enzimáticos
/
Indóis
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article