Novel 3-galloylamido-N′-substituted-2,6-piperidinedione-N-acetam ide peptidomimeties as metalloproteinase inhibitors

作者：Li, Qianbin; Fang, Hao; Xu, Wenfang^*

来源：Bioorganic & Medicinal Chemistry Letters, 2007, 17(10): 2935-2938.

DOI：10.1016/j.bmcl.2006.12.095

• aminopeptidase N
• matrix metalloproteinase
• peptidomimetics
• conformational constraint

Both of aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. Novel potent peptidomimetic inhibitors, containing 3-galloylamido-N'-substituted-2, 6-piperidinedione-N-acetamide, have been designed and synthesized according to the conformational constraint strategy. The preliminary biological test showed that most of the compounds displayed high inhibitory activity against MMP-2 and low activity against APN except compounds 6 (IC50 = 3.1 mu M) and 41 (IC50 = 5.2 mu M) which exhibit similar potency to Bestatin (IC50 = 2.4 mu M).

• 出版日期2007-5-15
• 单位山东大学; 河北医科大学