Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517.
Bioorg Med Chem Lett
; 17(14): 3819-25, 2007 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-17544272
ABSTRACT
Based on the lead compound BX-517, a series of C-4' substituted indolinones have been synthesized and evaluated for PDK1 inhibition. Modification at C-4' of the pyrrole afforded potent compounds (7b and 7d) with improved solubility and ADME properties. In this letter, we describe the synthesis, selectivity profile, and pharmacokinetic data of selected compounds.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ureia
/
Proteínas Serina-Treonina Quinases
/
Inibidores de Proteínas Quinases
/
Indóis
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2007
Tipo de documento:
Article