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Sunderland Repository records the research produced by the University of Sunderland including practice-based research and theses.

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold

Hardcastle, IR, Ahmed, Shafiq, Atkins, H, 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, HM and Lunec, J (2006) Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. J Med Chem, 49 (21). pp. 6209-6221.

Item Type: Article


From a set of weakly potent lead compounds, using in silico screening and small library synthesis, a series of 2-alkyl-3-aryl-3-alkoxyisoindolinones has been identified as inhibitors of the MDM2-p53 interaction. Two of the most potent compounds, 2-benzyl-3-(4-chlorophenyl)-3-(3-hydroxypropoxy)-2,3-dihydroisoindol-1-one (76; IC(50) = 15.9 +/- 0.8 microM) and 3-(4-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxybenzyloxy)-2-propyl-2,3-dihydroisoindol-1-one (79; IC(50) = 5.3 +/- 0.9 microM), induced p53-dependent gene transcription, in a dose-dependent manner, in the MDM2 amplified, SJSA human sarcoma cell line.

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More Information

Depositing User: Paula Normington


Item ID: 6014

Users with ORCIDS

ORCID for Shafiq Ahmed: ORCID iD

Catalogue record

Date Deposited: 17 Feb 2016 12:39
Last Modified: 18 Dec 2019 15:38


Author: Shafiq Ahmed ORCID iD
Author: IR Hardcastle
Author: H Atkins
Author: G Farnie
Author: BT Golding
Author: RJ Griffin
Author: S Guyenne
Author: C Hutton
Author: P Kallblad
Author: SJ Kemp
Author: MS Kitching
Author: DR Newell
Author: S Norbedo
Author: JS Northen
Author: RJ Reid
Author: K Saravanan
Author: HM Willems
Author: J Lunec

University Divisions

Faculty of Health Sciences and Wellbeing
Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences



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