2013
DOI: 10.2174/1573406411309040012
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Synthesis and Biological Evaluation of Novel Pyrimido[4,5-b]quinoline-2,4- dione Derivatives as MDM2 Ubiquitin Ligase Inhibitors

Abstract: 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-… Show more

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“…In line with ongoing research into the anticancer potential of pyrimido [4,5-b]quinoline-2,4-diones, several studies i. e. Dou et al [27] have explored their cytotoxic activity against various human cancer cell lines. The results were encouraging, with some compounds demonstrating potent antitumor effects.…”
Section: Introductionmentioning
confidence: 99%
“…In line with ongoing research into the anticancer potential of pyrimido [4,5-b]quinoline-2,4-diones, several studies i. e. Dou et al [27] have explored their cytotoxic activity against various human cancer cell lines. The results were encouraging, with some compounds demonstrating potent antitumor effects.…”
Section: Introductionmentioning
confidence: 99%