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

被引:34
作者
Brault, Laurent [1 ]
Denance, Mickael [1 ]
Banaszak, Estelle [1 ]
El Maadidi, Souhayla [1 ]
Battaglia, Eric [1 ]
Bagrel, Denyse [1 ]
Samadi, Mohammad [1 ]
机构
[1] Univ Paul Verlaine, LIMBP, F-57078 Metz, France
关键词
Barton decarboxylation; maleic anhydride; Cdc25; inhibition;
D O I
10.1016/j.ejmech.2006.09.014
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:243 / 247
页数:5
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