Development of Synthetic Aminopeptidase N/CD13 Inhibitors to Overcome Cancer Metastasis and Angiogenesis
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- 作者：Li Su ; Jiangying Cao ; Yuping Jia ; Xiaonan Zhang ; Hao Fang ; Wenfang Xu
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：December 13, 2012
- 年：2012
- 卷：3
- 期：12
- 页码：959-964
- 全文大小：367K
- 年卷期：v.3,no.12(December 13, 2012)
- ISSN：1948-5875
文摘
Cancer metastasis is a major barrier to its treatment and an important cause of patient death. Antimetastatic agents hold promise for patients with advanced metastatic tumors. Aminopeptidase N/CD13 (APN) is being pursued by many as an important target against cancer metastasis and angiogenesis, but there are few reports on the in vivo evaluation of synthetic APN inhibitors. Herein, a series of compounds targeting APN were synthesized and evaluated for their antimetastasis and antiangiogenesis potency both in vitro and in vivo. Excitingly, compounds 4m, 4t, and 4cc, with the most potent APN inhibitory activities, displayed significant antimetastasis and antiangiogenesis effects in vitro and in vivo, suggesting that those synthetic APN inhibitors have the potential to overcome cancer metastasis and angiogenesis.