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

L Brault, M Denancé, E Banaszak, S El Maadidi…

Index: Brault, Laurent; Denance, Mickael; Banaszak, Estelle; El Maadidi, Souhayla; Battaglia, Eric; Bagrel, Denyse; Samadi, Mohammad European Journal of Medicinal Chemistry, 2007 , vol. 42, # 2 p. 243 - 247

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Citation Number: 38

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 C9, to reach the optimal activity with a C17 chain length.