Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation

作者：Li, Qianbin^*; Fang, Hao; Wang, Xuejian; Hu, Gaoyun; Wang, Qiang; Xu, Wenfang

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(2): 850-853.

DOI：10.1016/j.bmcl.2011.12.048

• Aminopeptidase N
• Synthesis
• Peptidomimetics
• 2,5-Pyrrolidinedione
• Anti-tumor

A series of novel aminopeptidase N inhibitors with 2,5-pyrrolidinedione scaffold were chemically synthesized. Their preliminary biological activities in enzyme kinetics and cell assay in vitro and anti-metastasis profile in vivo were also evaluated. The results indicated that all the compounds displayed potent inhibitory activity against aminopeptidase N. Compound 8f inhibited aminopeptidase N activity with IC50 value of 1.0 mu M and displayed better activity profile in vivo than that of bestatin.

• 出版日期2012-1-15
• 单位中南民族大学; 中南大学; 山东大学; 河北医科大学