7269-03-6Relevant articles and documents
Synthesis and biological evaluation of novel pyrimido[4,5-b]quinoline-2,4- dione derivatives as MDM2 ubiquitin ligase inhibitors
Dou, Xiaoxue,Li, Xin,Tao, Liu,Hu, Chunqi,Zhang, Lei,He, Qiaojun,Yang, Bo,Hu, Yongzhou
, p. 581 - 587 (2013/07/28)
A series of pyrimido[4,5-b]quinoline-2,4-dione derivatives was synthesized and evaluated for their cytotoxic activities in vitro against five human cancer cell lines. Selected compounds were tested for their MDM2 E3 ligase inhibitory activities and p53-MDM2 binding inhibitory activities. Among tested compounds, four sulfur-containing compounds (4-7) displayed enhanced cytotoxic activities and better MDM2 E3 ligase inhibitoty activities in comparison with that of HLI98c. Three compounds (4-6) showed better p53-MDM2 binding inhibitory potency with IC50 values ranging from 1.3 μM to 9.0 μM.
Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells
Wilson, Jennifer M.,Henderson, Graham,Black, Fiona,Sutherland, Andrew,Ludwig, Robert L.,Vousden, Karen H.,Robins, David J.
, p. 77 - 86 (2007/10/03)
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.
