pb-12 and Neoplasms

Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2-p53 protein-protein interaction has been pursued as a new cancer therapeutic strategy. In recent years, potent, selective, and efficacious MDM2 inhibitors have been successfully obtained and seven such compounds have been advanced into early phase clinical trials for the treatment of human cancers. Here, we review the design, synthesis, properties, preclinical, and clinical studies of these clinical-stage MDM2 inhibitors.

Topics: Animals; Clinical Trials as Topic; Enzyme Inhibitors; Humans; Models, Molecular; Molecular Structure; Neoplasms; Protein Binding; Proto-Oncogene Proteins c-mdm2; Small Molecule Libraries; Structure-Activity Relationship; Tumor Suppressor Protein p53