1268684-06-5Relevant 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)
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.
CONDENSED HETEROCYCLIC COMPOUND
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Paragraph 0195-0200, (2017/11/08)
A compound represented by the general formula (I) [R1 represents a C1-6 alkyl group, a halogen atom, or the like; A represents a phenylene group, or the like; X represents —CH(R3)—, —O—, —NH—, or the like; Y represents —O—, —NH—, —N═, or —S—; . . . represents a single bond or double bond; n represents 1 to 3; R2 represents a C1-6 alkyl group, a C1-6 alkoxy group, or the like; and R3 represents hydrogen atom, a C1-6 alkyl group, or the like], or a salt thereof which has a blood LDL cholesterol-reducing action, and is useful as an active ingredient of medicaments.
