Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13

  • Bioorg Med Chem. 2009 Oct 15;17(20):7398-404. doi: 10.1016/j.bmc.2009.07.014.
Yingzi Liu  1 ,  Luqing Shang ,  Hao Fang ,  Huawei Zhu ,  Jiajia Mu ,  Qiang Wang ,  Xuejian Wang ,  Yumei Yuan ,  Wenfang Xu
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
PMID: 19782572 DOI: 10.1016/j.bmc.2009.07.014
Abstract

A series of novel derivatives of N-cinnamoyl-l-aspartic acid were designed, synthesized, and assayed for their inhibitory activities against Aminopeptidase N. The preliminary biological assay showed that compound 8c has the most potent inhibitory activity against APN with an IC(50) of 11.1+/-0.9 microM, this could be used as the lead compound in future research on Anticancer agents.