5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2

MP Dickens, P Roxburgh, A Hock, M Mezna…

Index: Dickens, Michael P.; Roxburgh, Patricia; Hock, Andreas; Mezna, Mokdad; Kellam, Barrie; Vousden, Karen H.; Fischer, Peter M. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 22 p. 6868 - 6877

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Citation Number: 2

Abstract

Abstract Based on previous reports of certain 5-deazaflavin derivatives being capable of activating the tumour suppressor p53 in cancer cells through inhibition of the p53-specific ubiquitin E3 ligase HDM2, we have conducted an structure–activity relationship (SAR) analysis through systematic modification of the 5-deazaflavin template. This analysis shows that HDM2-inhibitory activity depends on a combination of factors. The most active ...