| Literature DB >> 15713419 |
Ian R Hardcastle1, Shafiq U Ahmed, Helen Atkins, A Hilary Calvert, Nicola J Curtin, Gillian Farnie, Bernard T Golding, Roger J Griffin, Sabrina Guyenne, Claire Hutton, Per Källblad, Stuart J Kemp, Martin S Kitching, David R Newell, Stefano Norbedo, Julian S Northen, Rebecca J Reid, K Saravanan, Henriëtte M G Willems, John Lunec.
Abstract
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.Entities:
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Year: 2005 PMID： 15713419 DOI： 10.1016/j.bmcl.2004.12.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823