1268680-89-2Relevant 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.
TETRA-SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR USE AS MDM2 AND/OR MDM4 MODULATORS
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Page/Page column 164, (2011/04/14)
The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C-H, N-H or N, wherein the total number of nitrogen atoms represented by X1/su
