1428905-31-0Relevant articles and documents
Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach
Zaytsev, Andrey,Dodd, Barry,Magnani, Matteo,Ghiron, Chiara,Golding, Bernard T.,Griffin, Roger J.,Liu, Junfeng,Lu, Xiaohong,Micco, Iolanda,Newell, David R.,Padova, Alessandro,Robertson, Graeme,Lunec, John,Hardcastle, Ian R.
, p. 180 - 189 (2015)
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.