Discovery of a novel series of 4-quinolone JNK inhibitors.
Bioorg Med Chem Lett
; 22(24): 7381-7, 2012 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-23142618
ABSTRACT
A novel series of highly selective JNK inhibitors based on the 4-quinolone scaffold was designed and synthesized. Structure based drug design was utilized to guide the compound design as well as improvements in the physicochemical properties of the series. Compound (13c) has an IC(50) of 62/170 nM for JNK1/2, excellent kinase selectivity and impressive efficacy in a rodent asthma model.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
4-Quinolonas
/
Proteínas Quinases JNK Ativadas por Mitógeno
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Inibidores de Proteínas Quinases
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Descoberta de Drogas
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article