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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.
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
URL: http://dx.doi.org/10.1016/j.bmcl.2004.12.061
DOI: 10.1016/j.bmcl.2004.12.061
PubMed id: 15713419
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