Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction
作者： Ian R Hardcastle , Shafiq U Ahmed , Helen Atkins , A Hilary Calvert , Nicola J Curtin
DOI: 10.1016/J.BMCL.2004.12.061
关键词:
摘要: A series of 2-N-alkyl-3-aryl-3-alkoxyisoindolinones has been synthesised and evaluated as inhibitors 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 5.3 +/- 0.9 microM in ELISA assay, induced p53-dependent gene transcription a dose-dependent manner, SJSA human sarcoma cell line.
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