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  2. Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases

Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases

  • Eur J Med Chem. 2007 Feb;42(2):243-7. doi: 10.1016/j.ejmech.2006.09.014.
Laurent Brault 1 Mickaël Denancé Estelle Banaszak Souhayla El Maadidi Eric Battaglia Denyse Bagrel Mohammad Samadi
Affiliations

Affiliation

  • 1 LIMBP, Université Paul Verlaine-Metz, Metz Technopôle, 57078 Metz, France.
Abstract

An efficient synthesis of dialkylsubstituted maleic anhydrides 1a-j is described. The inhibitory potential of these original anhydride derivatives was tested toward the three human isoforms A, B and C of dual specific phosphatases Cdc25. A micromolar range inhibition of Cdc25s was observed with the maleic anhydrides bearing simple alkyl side chains longer than C(9), to reach the optimal activity with a C(17) chain length.

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