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

Hardcastle, IR, Ahmed, Shafiq, Atkins, H, Calvert, AH, Curtin, NJ, Farnie, G, Golding, BT, Griffin, RJ, Guyenne, S, Hutton, C, Kallblad, P, Kemp, SJ, Kitching, MS, Newell, DR, Norbedo, S, Northen, JS, Reid, RJ, Saravanan, K, Willems, H and Lunec, J (2005) Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction. Bioorganic & Medicinal Chemistry Letters, 15 (5). pp. 1515-1520.

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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.

Item Type: Article
Subjects: Sciences
Divisions: Faculty of Applied Sciences
Faculty of Applied Sciences > Department of Pharmacy Health and Wellbeing
Health Sciences and Wellbeing Beacon
Depositing User: Paula Normington
Date Deposited: 17 Feb 2016 12:41
Last Modified: 17 Feb 2016 12:41

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