This Letter describes the further development and SAR exploration of a novel series of Legumain inhibitors. Based upon a previously identified Legumain inhibitor from our group, we explored the SAR of the carbamate phenyl ring system to probe the P3 pocket of the enzyme. This led to the identification of a sub-nanomolar inhibitor of Legumain.
Higgins, C., Bouazzaoui, S., Gaddale Devanna, K., D'Costa, Z., Templeman, A., O'Rourke, M., Young, A., Scott, C., Harrison, T., Mullan, P., & Williams, R. (2014). P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(11), 2521-2524. https://doi.org/10.1016/j.bmcl.2014.04.002