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A series of 2-N-alkyl-3-aryl-3-alkoxyisoindolinones has been synthesised and evaluated as inhibitors of the MDM2-p53 interaction. The most potent compound, 3-(4-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxybenzyloxy)-2-propyl-2,3-dihydroisoindol-1-one (NU8231), exhibited an IC50 of 5.3 +/- 0.9 microM in an ELISA assay, and induced p53-dependent gene transcription in a dose-dependent manner, in the SJSA human sarcoma cell line.

Type

Journal article

Journal

Bioorganic & medicinal chemistry letters

Publication Date

03/2005

Volume

15

Pages

1515 - 1520

Addresses

Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, University of Newcastle upon Tyne, Newcastle upon Tyne, NE1 7RU, UK. i.r.hardcastle@ncl.ac.uk

Keywords

Cell Line, Tumor, Humans, Indoles, Proto-Oncogene Proteins, Nuclear Proteins, Transcription, Genetic, Molecular Structure, Protein Binding, Structure-Activity Relationship, Dose-Response Relationship, Drug, Models, Molecular, Tumor Suppressor Protein p53, Proto-Oncogene Proteins c-mdm2