2. Academic Validation
  3. Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione

Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione

  • Bioorg Med Chem. 2010 Aug 15;18(16):5981-7. doi: 10.1016/j.bmc.2010.06.078.
Xiaopan Zhang 1,  Hao Fang,  Huawei Zhu,  Xuejian Wang,  Lei Zhang,  Minyong Li,  Qianbin Li,  Yumei Yuan,  Wenfang Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.
PMID: 20637634 DOI: 10.1016/j.bmc.2010.06.078
Abstract

Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel APN inhibitors with 3-phenylalanyl-N'-substituted-2,6-piperidinedione scaffold. The results showed that compound 7c had the most potent inhibitory activity against APN with the IC(50) value to 5.00 +/-3.17 microM, which could be used as the lead compound in the future for Anticancer agent research.

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