Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles.
Bioorg Med Chem Lett
; 19(9): 2461-3, 2009 May 01.
Article
em En
| MEDLINE
| ID: mdl-19345579
ABSTRACT
A series of 4-indolylamino-5-phenyl-3-pyridinecarbonitrile inhibitors of PKCtheta were synthesized as potential anti-inflammatory agents. The effects of specific substitution on the 5-phenyl moiety and variations of the positional isomers of the 4-indolylamino substituent were explored. This study led to the discovery of compound 12d, which had an IC(50) value of 18nM for the inhibition of PKCtheta.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Proteína Quinase C
/
Inibidores de Proteínas Quinases
/
Isoenzimas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Estados Unidos