N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.
Bioorg Med Chem Lett
; 20(24): 7503-6, 2010 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-21106457
ABSTRACT
We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors (9) targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Bencimidazoles
/
Proteínas HSP90 de Choque Térmico
Límite:
Humans
Idioma:
En
Año:
2010
Tipo del documento:
Article