Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.
Bioorg Med Chem Lett
; 20(7): 2229-33, 2010 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-20189383
ABSTRACT
A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Tiazóis
/
Proteínas Inibidoras de Apoptose
/
Amidas
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Estados Unidos