1256581-66-4Relevant articles and documents
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors
Holzer, Philipp,Masuya, Keiichi,Furet, Pascal,Kallen, Joerg,Valat-Stachyra, Therese,Ferretti, Stéphane,Berghausen, Joerg,Bouisset-Leonard, Michèle,Buschmann, Nicole,Pissot-Soldermann, Carole,Rynn, Caroline,Ruetz, Stephan,Stutz, Stefan,Chène, Patrick,Jeay, Sébastien,Gessier, Francois
supporting information, p. 6348 - 6358 (2015/09/07)
(Figure Presented). As a result of our efforts to discover novel p53:MDM2 protein-protein interaction inhibitors useful for treating cancer, the potent and selective MDM2 inhibitor NVP-CGM097 (1) with an excellent in vivo profile was selected as a clinical candidate and is currently in phase 1 clinical development. This article provides an overview of the discovery of this new clinical p53:MDM2 inhibitor. The following aspects are addressed: mechanism of action, scientific rationale, binding mode, medicinal chemistry, pharmacokinetic and pharmacodynamic properties, and in vivo pharmacology/toxicology in preclinical species.
Crystalline form of an inhibitor of MDM2/4 and p53 interaction
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Page/Page column 13-14, (2012/06/01)
A crystalline form of (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one, which is useful in the treatment of a disease or disorder associated with the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively,