Potent blockers of the monocarboxylate transporter MCT1: Novel immunomodulatory compounds

A novel series of potent blockers of the monocarboxylate transporter, MCT1, is disclosed. From very potent but lipophilic lead compounds, systematic changes to all parts of the molecule, targeting reduction in log D, afforded compounds with significantly improved overall properties. These compounds show potent immunomodulatory activity.

The synthesis and properties of a novel series of potent blockers of the monocarboxylate transporter, MCT1, are described. These compounds, exemplified by 30, show potent immunomodulatory activity.Figure optionsDownload as PowerPoint slide