2. Academic Validation
  3. Novel naphthoquinone and quinolinedione inhibitors of CDC25 phosphatase activity with antiproliferative properties

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

  • Bioorg Med Chem. 2008 Oct 1;16(19):9040-9. doi: 10.1016/j.bmc.2008.08.009.
Emmanuelle Braud 1,  Mary-Lorène Goddard,  Stéphanie Kolb,  Marie-Priscille Brun,  Odile Mondésert,  Muriel Quaranta,  Nohad Gresh,  Bernard Ducommun,  Christiane Garbay
Affiliations

Affiliation

  • 1 Université Paris Descartes, UFR biomédicale, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, 45 rue des Saints-Pères, Paris F-75006, France.
PMID: 18789703 DOI: 10.1016/j.bmc.2008.08.009
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 IC(50) values in the 10 microM range, and are cytotoxic against HeLa cells.

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