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J Med Chem. 2006 Jun 29;49(13):3759-62.

Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.

Author information

1
Comprehensive Cancer Center and Department of Medicinal Chemistry, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, USA.

Abstract

An integrated, virtual database screening strategy has led to 7-[anilino(phenyl)methyl]-2-methyl-8-quinolinol (4, NSC 66811) as a novel inhibitor of the murine double minute 2 (MDM2)-p53 interaction. This quinolinol binds to MDM2 with a Ki of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction. It mimics three p53 residues critical in the binding to MDM2 and represents a promising new class of non-peptide inhibitors of the MDM2-p53 interaction.

PMID:
16789731
DOI:
10.1021/jm060023+
[Indexed for MEDLINE]

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