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Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach.
Andrey Zaytsev
1 ,
Barry Dodd
1 ,
Matteo Magnani
2 ,
Chiara Ghiron
2 ,
Bernard T Golding
1 ,
Roger J Griffin
1 ,
Junfeng Liu
3 ,
Xiaohong Lu
3 ,
Iolanda Micco
2 ,
David R Newell
3 ,
Alessandro Padova
2 ,
Graeme Robertson
2 ,
John Lunec
3 ,
Ian R Hardcastle
1
Aug 2015
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Abstract
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.