Title of article
Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties Original Research Article
Author/Authors
Emmanuelle Braud، نويسنده , , Mary-Lorène Goddard، نويسنده , , Stéphanie Kolb، نويسنده , , Marie-Priscille Brun، نويسنده , , Odile Mondésert، نويسنده , , Muriel Quaranta، نويسنده , , Nohad Gresh، نويسنده , , Bernard Ducommun، نويسنده , , Christiane Garbay، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
10
From page
9040
To page
9049
Abstract
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.
Keywords
Cancer , Phosphatase CDC25 , Cell cycle regulation , Quinone derivatives
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306927
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