Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.
Bioorg Med Chem Lett
; 19(3): 766-9, 2009 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-19111463
ABSTRACT
Thieno[2,3-b]pyridine-5-carbonitrile 16 with a 4-methyl-5-indolylamine at C-4 and a 5-methoxy-2-(dimethylamino)-methylphenyl group at C-2 had an IC(50) value of 16 nM for the inhibition of PKCtheta. While moderate inhibition of PKCdelta was also observed (IC(50)=130 nM), 16 had IC(50) values of greater than 5 microM against Lyn and other members of the Src kinase family.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Proteína Quinase C
/
Química Farmacêutica
/
Indóis
/
Isoenzimas
/
Nitrilas
Limite:
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