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.

Item Type:	Article

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.

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More Information

Depositing User: Paula Normington

Identifiers

Item ID: 6015

Identification Number: 10.1016/j.bmcl.2004.12.061

URI: http://sure.sunderland.ac.uk/id/eprint/6015

Users with ORCIDS

ORCID for Shafiq Ahmed:

orcid.org/0000-0001-8701-6889

Catalogue record

Date Deposited: 17 Feb 2016 12:41

Last Modified: 04 Jun 2025 17:41

Contributors

Author:	Shafiq Ahmed
Author:	IR Hardcastle
Author:	H Atkins
Author:	AH Calvert
Author:	NJ Curtin
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:	H Willems
Author:	J Lunec