Novel aminopeptidase N inhibitors derived from 1, 3, 4-thiadiazole scaffold

…, SH Li, HM Huang, G Li, F Xiong, X Mai, HW Zhu…

Index: Tu, GuoGang; Li, ShaoHua; Huang, HuiMing; Li, Gang; Xiong, Fang; Mai, Xi; Zhu, HuaWei; Kuang, BinHai; Xu, Wen Fang Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6663 - 6668

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Citation Number: 47

Abstract

The aminopeptidase N (APN/CD13), overexpressed in tumor cells, plays a critical role in angiogenesis. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1, 3, 4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC50 values in the micromol rang.