Synthesis and p38 Inhibitory Activity of Some Novel Substituted N,N'-Diarylurea Derivatives.
Molecules
; 21(5)2016 May 23.
Article
en En
| MEDLINE
| ID: mdl-27223276
ABSTRACT
We have identified a novel series of substituted N,N'-diarylurea p38α inhibitors. The inhibitory activity of the target compounds against the enzyme p38α, MAPKAPK2 in BHK cells, TNF-α release in LPS-stimulated THP-1 cells and p38α binding experiments were tested. Among these compounds, 25a inhibited the p38α enzyme with an IC50 value of 0.47 nM and a KD value of 1.54 × 10(-8) and appears to be the most promising one in the series.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Urea
/
Factor de Necrosis Tumoral alfa
/
Proteínas Serina-Treonina Quinasas
/
Proteínas Quinasas p38 Activadas por Mitógenos
/
Péptidos y Proteínas de Señalización Intracelular
/
Inhibidores Enzimáticos
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Molecules
Asunto de la revista:
BIOLOGIA
Año:
2016
Tipo del documento:
Article
País de afiliación:
China