Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties

CDC25 phosphatases are considered as attractive targets for anti-cancer therapy. To date, quinone derivatives are among the most potent inhibitors of CDC25 phosphatase activity. We present in this paper the synthesis and the biological evaluation of new quinolinedione and naphthoquinone derivatives, containing carboxylic or malonic acids groups introduced to mimic the role of the phosphate moieties of Cyclin-Dependent Kinase complexes. The most efficient compounds show inhibitory activity against CDC25B with IC50 values in the 10 μM range, and are cytotoxic against HeLa cells.

Novel naphthoquinone and quinolinedione derivatives were evaluated for their inhibitory activity toward CDC25 phosphatase activity. These compounds also display cytotoxic activity against HeLa cells.Figure optionsDownload as PowerPoint slide