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Lookup NU author(s): Dr Ian HardcastleORCiD, Dr Shafiq Ahmed, Helen Atkins, Gillian Farnie, Emeritus Professor Bernard Golding, Professor Roger Griffin, Dr Sabrina Guyenne, Dr Claire Hutton, Stuart Kemp, Professor Herbie Newell, Dr Stefano Norbedo, Dr Julian Scott Northen, Rebecca Reid, Dr Kappusamy Saravanan, Professor John LunecORCiD
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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; IC50 = 15.9 ± 0.8 μM) and 3-(4-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxybenzyloxy)-2-propyl-2, 3-dihydroisoindol-1-one (79; IC50 = 5.3 ± 0.9 μM), induced p53-dependent gene transcription, in a dose-dependent manner, in the MDM2 amplified, SJSA human sarcoma cell line. © 2006 American Chemical Society.
Author(s): Hardcastle, I.R., Ahmed, S., Atkins, H., Farnie, G., Golding, B.T., Griffin, R.J., Guyenne, S., Hutton,C., Källblad, P., Kemp, S., Kitching, M.S., Newell, D.R., Norbedo, S., Northen, J.S., Reid, R.J., Saravanan, K., Willems, H., Lunec, J.
Publication type: Article
Publication status: Published
Journal: Journal of Medicinal Chemistry
Year: 2006
Volume: 49
Issue: 21
Pages: 6209-6221
Print publication date: 01/10/2006
ISSN (print): 0022-2623
ISSN (electronic): 1520-4804
URL: http://dx.doi.org/10.1021/jm0601194
DOI: 10.1021/jm0601194
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