Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I)

作者：Li, Xun; Wang, Junli; Li, Jinpei; Wu, Jifeng; Li, Yonggang; Zhu, Huawei; Fan, Ruifang; Xu, Wenfang^*

来源：Bioorganic & Medicinal Chemistry, 2009, 17(8): 3053-3060.

DOI：10.1016/j.bmc.2009.02.063

• L-iso-Glutamine derivatives
• Antineoplaston AS2-5
• APN inhibitors
• Peptidomimetics
• Anti-tumor

Overexpression of zinc-dependent metalloproteinase, aminopeptidase N (APN/CD13), is considered to be involved in the process of tumor invasion and metastasis. Herein we describe the synthesis and in vitro enzymatic inhibition assay of antineoplaston AS2-5 scaffold peptidomimetic compounds. The results demonstrated that most of these L-iso-glutamine derivatives displayed selective inhibitory activity against APN as compared with MMP-2, with IC50 values in the micromole range. The structure-activity relationships were also briefly discussed.

• 出版日期2009-4-15
• 单位聊城市人民医院; 山东大学