Li Shao-hua, Li Gang, Huang Hui-ming, Xiong Fang, Liu Cheng-mei, Tu Guo-gang
State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, PR China.
Arch Pharm Res. 2008 Oct;31(10):1231-9. doi: 10.1007/s12272-001-2101-6. Epub 2008 Oct 29.
Both the aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. A series of novel peptide-like derivatives were designed and synthesized as antitumor agents. Their structures were confirmed by IR, MS, and (1)H-NMR. These compounds exhibited potent inhibitory activities against APN and low activity against MMP in vitro. The derivatives with methoxy group show better activities than those with other substituted group and could be used as lead compounds for exploring new APN inhibitors in the future.
氨肽酶N（APN）和基质金属蛋白酶（MMP）都是肿瘤侵袭和血管生成过程中必不可少的金属肽酶。设计并合成了一系列新型肽样衍生物作为抗肿瘤药物。通过红外光谱（IR）、质谱（MS）和氢核磁共振（¹H-NMR）对其结构进行了确证。这些化合物在体外对APN表现出强效抑制活性，而对MMP的活性较低。带有甲氧基的衍生物比带有其他取代基的衍生物表现出更好的活性，未来可作为探索新型APN抑制剂的先导化合物。
