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Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction

Lookup NU author(s): Dr Ian HardcastleORCiD, Dr Shafiq Ahmed, Professor Alan Calvert, Professor Nicola CurtinORCiD, Gillian Farnie, Emeritus Professor Bernard Golding, Professor Roger Griffin, Sabrina Guyenne, Dr Claire Hutton, Stuart Kemp, Professor Herbie Newell, Dr Stefano Norbedo, Dr Julian Scott Northen, Rebecca Reid, Dr Kappusamy Saravanan, Professor John LunecORCiD



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 μM in an ELISA assay, and induced p53-dependent gene transcription in a dose-dependent manner, in the SJSA human sarcoma cell line. © 2005 Elsevier Ltd. All rights reserved.

Publication metadata

Author(s): Hardcastle I, Ahmed S, Atkins H, Calvert AH, Curtin NJ, Farnie G, Golding BT, Griffin R, Guyenne S, Hutton C, Källblad P, Kemp S, Kitching M, Newell D, Norbedo S, Northen J, Reid R, Saravanan K, Willems H, Lunec J

Publication type: Article

Publication status: Published

Journal: Bioorganic and Medicinal Chemistry Letters

Year: 2005

Volume: 15

Issue: 5

Pages: 1515-1520

Print publication date: 01/03/2005

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405


DOI: 10.1016/j.bmcl.2004.12.061

PubMed id: 15713419


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