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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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.

Item Type: Article
Subjects: Sciences
Divisions: Faculty of Health Sciences and Wellbeing
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences
Depositing User: Paula Normington
Date Deposited: 17 Feb 2016 12:41
Last Modified: 18 Dec 2019 15:38
URI: http://sure.sunderland.ac.uk/id/eprint/6015
ORCID for Shafiq Ahmed: ORCID iD orcid.org/0000-0001-8701-6889

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