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Discovery of Potent and Selective p53-MDM2 Protein-Protein Interaction Inhibitors as Anticancer Drugs
1Novartis Institutes for BioMedical Research CH-4002 Basel;,
Abstract:
As a result of our persistent efforts to discover novel inhibitors of the p53-MDM2 protein-protein interaction useful for the treatment of cancer, the potent and selective MDM2 inhibitors NVP-CGM097 and NVP-HDM201 with excellent in vitro and in vivo profile were selected as clinical candidates and are currently in phase 1 clinical development. This short review article provides a summary of the program history, the applied pharmacophore model and the discovery story of these novel p53-MDM2 inhibitor investigational drugs.
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