Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors

Journal of Medicinal Chemistry

Volumn 58, Issue 16, 2015, Pages 6348-6358

  Holzer, Philipp ^a   Masuya, Keiichi ^a,b   Furet, Pascal ^a   Kallen, Joerg ^a   Valat Stachyra, Therese ^a   Ferretti, Stéphane ^a   Berghausen, Joerg ^a   Bouisset Leonard, Michèle ^a   Buschmann, Nicole ^a   Pissot Soldermann, Carole ^a   Rynn, Caroline ^a   Ruetz, Stephan ^a   Stutz, Stefan ^a   Chène, Patrick ^a   Jeay, Sébastien ^a   Gessier, Francois ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b PEPTIDREAM INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; DIHYDROISOQUINOLINONE DERIVATIVE; MESSENGER RNA; PROTEIN MDM2; PROTEIN P53; UNCLASSIFIED DRUG; ISOQUINOLINE DERIVATIVE; NVP-CGM097; PIPERAZINE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL PROLIFERATION; CELL PROLIFERATION ASSAY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; HISTOPATHOLOGY; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; ISOTHERMAL TITRATION CALORIMETRY; LIVER MICROSOME; METABOLIC CLEARANCE; MOLECULAR MODEL; MOUSE; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PLASMA PROTEIN BINDING; PROTEIN PROTEIN INTERACTION; RAT; STEREOISOMERISM; TIME-DEPENDENT INHIBITION; TISSUE DISTRIBUTION; TUMOR GROWTH; TUMOR REGRESSION; VOLUME OF DISTRIBUTION; VOLUME OF DISTRIBUTION AT STEADY-STATE; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG DEVELOPMENT; DRUG SCREENING; GENETICS; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CLINICAL TRIALS, PHASE I AS TOPIC; DRUG DISCOVERY; HUMANS; ISOQUINOLINES; PIPERAZINES; PROTO-ONCOGENE PROTEINS C-MDM2; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR SUPPRESSOR PROTEIN P53; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84940569947     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00810     Document Type: Article

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