Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors

作者：Shang, Luqing; Fang, Hao; Zhu, Huawei; Wang, Xuejian; Wang, Qiang; Mu, Jiajia; Wang, Binghe; Kishioka, Shiroh; Xu, Wenfang^*

来源：Bioorganic & Medicinal Chemistry, 2009, 17(7): 2775-2784.

DOI：10.1016/j.bmc.2009.02.034

• Aminopeptidase N inhibitor
• 3-Phenylpropane-1,2-diamine
• Tripeptide analogs
• Synthesis

Aminopeptidase N (APN), belonged to metalloproteinase, is an essential peptidase involved in the process of tumor invasion and metastasis. A series of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine were designed, synthesized and evaluated for their ability to inhibit APN. Preliminary activity evaluation showed that most of target compounds possessed potent inhibitory activities against APN. With in this series, compound A6 and B6 exhibited good potency with the IC50 values of 8.8 +/- 1.3 mu M and 8.6 +/- 1.1 mu M, respectively.

• 出版日期2009-4-1
• 单位山东大学