Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells

Wilson, J., Henderson, G., Black, F., Sutherland, A., Ludwig, R., Vousden, K. and Robins, D. (2007) Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells. Bioorganic and Medicinal Chemistry Letters, 15, pp. 77-86. (doi: 10.1016/j.bmc.2006.10.011)

Abstract

A family of 5-deazaflavin derivatives has been synthesised using a two-step convergent strategy. The biological activity of these compounds was evaluated in cells, by assessing their ability to stabilize and activate p53. These compounds may act as low molecular weight inhibitors of the E3 activity of HMD2 in tumours that retain wild-type p53. Importantly, we have demonstrated that the nitro group present in all three of the original lead compounds [1-3 (HL198C-E)] is not essential for observation of this biological activity

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Sutherland, Professor Andrew and Vousden, Karen and Robins, Prof David
• Authors: Wilson, J., Henderson, G., Black, F., Sutherland, A., Ludwig, R., Vousden, K., and Robins, D.
• College/School: College of Medical Veterinary and Life Sciences > School of Cancer Sciences; College of Science and Engineering > School of Chemistry
• Journal Name: Bioorganic and Medicinal Chemistry Letters
• ISSN: 0960-894X