Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, 44, West Culture Road, Ji'nan 250012, PR China.
Bioorg Med Chem. 2011 Oct 15;19(20):6015-25. doi: 10.1016/j.bmc.2011.08.041. Epub 2011 Aug 24.
A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ± 0.11 μM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ± 0.01 μM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.
设计、合成了一系列新型的 1,2,3,4-四氢异喹啉-3-羧酸衍生物，并测定了它们对氨基肽酶 N（APN/CD13）和 MMP-2 的活性。结果表明，大多数化合物对 APN 的抑制活性均高于 MMP-2。在这一系列化合物中，化合物 12h（IC50=6.28±0.11μM）对 APN 的抑制活性与 Bestatin（IC50=5.55±0.01μM）相似，可作为新型先导化合物用于未来 APN 抑制剂的开发，作为抗癌药物。
