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

JM Wilson, G Henderson, F Black, A Sutherland…

文献索引：Wilson, Jennifer M.; Henderson, Graham; Black, Fiona; Sutherland, Andrew; Ludwig, Robert L.; Vousden, Karen H.; Robins, David J. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 1 p. 77 - 86

全文：HTML全文

被引用次数: 37

摘要

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 ...