Design, synthesis and primary activity evaluation of L-arginine derivatives as amino-peptidase N/CD13 inhibitors.
Design, synthesis and primary activity evaluation of L-arginine derivatives as amino-peptidase N/CD13 inhibitors.
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DOI：
10.1016/j.bmc.2009.04.056
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发表时间：
2009-07-01
影响因子：
3.5
通讯作者：
Xu W
中科院分区：
文献类型：
--
作者：
Mou J;Fang H;Jing F;Wang Q;Liu Y;Zhu H;Shang L;Wang X;Xu W
设计、合成了一系列L精氨酸衍生物，并测定了它们对氨基肽酶N(APN/CD13)和金属蛋白酶-2(MMP2)的活性。结果表明，大部分化合物对APN具有较高的抑制活性，而对基质金属蛋白酶-2的抑制活性较低。设计、合成了一系列L精氨酸衍生物，并测定了它们对氨基肽酶N(APN/CD13)和金属蛋白酶-2(MMP2)的活性。结果表明，大部分化合物对APN具有较高的抑制活性，而对基质金属蛋白酶-2的抑制活性较低。其中，化合物5q和5s(IC50值分别为55.3和5.1gμM)的抑制活性与Bestatin(IC50值=33.8gμM)相近，可作为未来APN抑制剂作为抗癌药物开发的先导化合物。
A series of l-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. A series of l-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this series, two compounds 5q and 5s (IC50 = 5.3 and 5.1 μM) showed similar inhibitory activities compared with bestatin (IC50 = 3.8 μM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.
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影响因子：
1.6
作者：
Chung, MC;Lee, HJ;Kho, YH
通讯作者：
Kho, YH
影响因子：
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作者：
Egan, ME;Pearson, M;Caplan, MJ
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