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 |
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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.
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| Depositing User: Paula Normington |
Identifiers
| Item ID: 6015 |
| Identification Number: https://doi.org/10.1016/j.bmcl.2004.12.061 |
| URI: http://sure.sunderland.ac.uk/id/eprint/6015 |
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| Date Deposited: 17 Feb 2016 12:41 |
| Last Modified: 18 Dec 2019 15:38 |
| 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 |
University Divisions
Faculty of Health Sciences and WellbeingFaculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences
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