C1 and N5 derivatives of cerpegin: Synthesis of a new series based on structure-activity relationships to optimize their inhibitory effect on 20S proteasome

A new class of 20S proteasome inhibitors has been identified among C1 and N5 derivatives of cerpegin. The post-acid (PA) activity of the β1 subunit of the 20S proteasome was specifically inhibited at the micromolar range. In silico docking suggests a unique mode of binding for these molecules.