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

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 IC50 of 11.1 ± 0.9 μM, this could be used as the lead compound in future research on anticancer agents.

The compound 8c was built and docked into the active site of APN (PDB code: 2DQM) using Sybyl7.0. The docking result was showed by PyMOL.Figure optionsDownload as PowerPoint slide