Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors |
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| Authors: | Zhang Xiaopan Zhang Jian Zhang Lei Feng Jinghong Xu Yingying Yuan Yumei Fang Hao Xu Wenfang |
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| Institution: | Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, 44, West Culture Road, Ji'nan 250012, PR China. |
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| Abstract: | 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. |
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