Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.
Org Biomol Chem
; 10(15): 2928-33, 2012 Apr 21.
Article
em En
| MEDLINE
| ID: mdl-22395339
ABSTRACT
By conducting a structure-activity relationship study of the backbone of a series of oligoamide-foldamer-based α-helix mimetics of the Bak BH3 helix, we have identified especially potent inhibitors of Bcl-x(L). The most potent compound has a K(i) value of 94 nM in vitro, and single-digit micromolar IC(50) values against the proliferation of several Bcl-x(L)-overexpressing cancer cell lines.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Picolínicos
/
Benzamidas
/
Materiais Biomiméticos
/
Proteína bcl-X
/
Antineoplásicos
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Revista:
Org Biomol Chem
Ano de publicação:
2012
Tipo de documento:
Article