Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)

Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC50 value 15.5 ± 1.2 μM.

The most active compound 12i was built and docked into the active site of APN (PDB code: 2DQM) using Sybyl7.0. The docking result was showed by LIGPLOT.Figure optionsDownload as PowerPoint slide