1.
Chem Biol Drug Des
; 86(2): 180-9, 2015 Aug.
Artigo
em Inglês
| MEDLINE
| ID: mdl-25388787
RESUMO
Two libraries of substituted benzimidazoles were designed using a 'scaffold-hopping' approach based on reported MDM2-p53 inhibitors. Substituents were chosen following library enumeration and docking into an MDM2 X-ray structure. Benzimidazole libraries were prepared using an efficient solution-phase approach and screened for inhibition of the MDM2-p53 and MDMX-p53 protein-protein interactions. Key examples showed inhibitory activity against both targets.