Design, Synthesis, and Preliminary Activity Evaluation of Novel Peptidomimetics as Aminopeptidase N/CD13 Inhibitors

被引：10

作者：

Li, Xun ^{[1
]}

Wang, Junli ^{[1
]}

Zhang, Lei ^{[1
]}

Xu, Wenfang ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Jinan 250012, Shandong, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2011年 / 344卷 / 08期

关键词：

Aminopeptidase N inhibitor; Antiproliferative activity; APN/CD13; Peptidomimetics; ESCHERICHIA-COLI; INVASION; CANCER; TARGET; CELLS;

D O I：

10.1002/ardp.201100109

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a series of novel N-alpha-galloylated isoglutamic acid gamma-amide peptidomimetics is described. Their enzymatic inhibition against aminopeptidase N (APN/CD13) and matrix metalloproteinase-2 (MMP-2) was tested. The preliminary activity assay revealed that most of the compounds displayed selective inhibition against APN as compared with MMP-2, with IC(50) values in a micromolar range. Within this series, compound 4 (IC(50) = 10.2 +/- 0.9 mu M) demonstrated comparable APN inhibition as compared with the positive control bestatin (IC(50) = 13.1 +/- 0.7 mu M), which might be a promising lead for further molecular optimizations.

引用

页码：494 / 504

页数：11

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