Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction.
نویسندگان
چکیده
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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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 15 5 شماره
صفحات -
تاریخ انتشار 2005