1268684-03-2Relevant academic research and scientific papers
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction
Vaupel, Andrea,Bold, Guido,De Pover, Alain,Stachyra-Valat, Thérèse,Hergovich-Lisztwan, Joanna,Kallen, Joerg,Masuya, Keiichi,Furet, Pascal
, p. 2110 - 2114 (2014/05/06)
Capitalizing on crystal structure information obtained from a previous effort in the search for non peptide inhibitors of the p53-MDM2 interaction, we have discovered another new class of compounds able to disrupt this protein-protein interaction, an important target in oncology drug research. The new inhibitors, based on a tetra-substituted imidazole scaffold, have been optimized to low nanomolar potency in a biochemical assay following a structure-guided approach. An appropriate strategy has allowed us to translate the high biochemical potency in significant anti-proliferative activity on a p53-dependent MDM2 amplified cell line.
