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 μM and 8.6 ± 1.1 μM, respectively.

中文翻译：

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以三苯基类似物3-苯基丙烷-1,2-二胺为氨基肽酶N / CD13抑制剂的三肽类似物的设计，合成和SAR研究

氨肽酶N（APN）属于金属蛋白酶，是一种参与肿瘤侵袭和转移过程的必不可少的肽酶。设计，合成了一系列具有支架3-苯基丙烷-1,2-二胺的三肽类似物，并评估了它们抑制APN的能力。初步活性评估表明，大多数目标化合物均具有针对APN的有效抑制活性。在该系列中，化合物A6和B6表现出良好的效价，IC ₅₀值分别为8.8±1.3μM和8.6±1.1μM。