Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases
作者:Laurent Brault、Mickaël Denancé、Estelle Banaszak、Souhayla El Maadidi、Eric Battaglia、Denyse Bagrel、Mohammad Samadi
DOI:10.1016/j.ejmech.2006.09.014
日期:2007.2
An efficient synthesis of dialkyl substituted 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. (c) 2006 Elsevier Masson SAS. All rights reserved.