Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
Bioorg Med Chem Lett
; 21(6): 1719-23, 2011 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-21316221
ABSTRACT
Quinazoline 3 was discovered as a novel c-jun N-terminal kinase (JNK) inhibitor with good brain penetration and pharmacokinetic (PK) properties. A number of analogs which were potent both in the biochemical and cellular assays were discovered. Quinazoline 13a was found to be a potent JNK3 inhibitor (IC(50)=40 nM), with >500-fold selectivity over p38, and had good PK and brain penetration properties. With these properties, 13a is considered a potential candidate for in vivo evaluation.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinazolinas
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Proteínas Quinases JNK Ativadas por Mitógeno
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Inibidores de Proteínas Quinases
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article