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Beschreibung

A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53-MDM2 interaction and p53 ubiquitination and induces p53-dependent apoptosis in tumor cells expressing wild-type p53. Shown to restore the tumor suppressor function of p53 by inducing its accumulation in HCT116 colon carcinoma cells (~0.1 µ,M) and in p53-positive SCID mice xenografted with HCT116 cells (0.1, 1 or 10 mg/kg, ip) in vivo.