| Literature DB >> 25388787 |
Andrey Zaytsev1, Barry Dodd1, Matteo Magnani2, Chiara Ghiron2, Bernard T Golding1, Roger J Griffin1, Junfeng Liu3, Xiaohong Lu3, Iolanda Micco2, David R Newell3, Alessandro Padova2, Graeme Robertson2, John Lunec3, Ian R Hardcastle1.
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.Entities:
Keywords: drug design; drug discovery; protein-protein interaction; structure-based drug design; virtual screening
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Year: 2014 PMID： 25388787 DOI： 10.1111/cbdd.12474
Source DB: PubMed Journal: Chem Biol Drug Des ISSN： 1747-0277 Impact factor: 2.817