Monocarboxylate transporters (MCTs) are 12-transmembrane proteins that direct small monocarboxylates across the plasma cell membranes. Two isoforms, MCT1 and MCT4, are especially abundant in tumor cells, where lactate is produced through glycolysis. Recently, MCT1 inhibition was shown to have promise for the treating MCT1-expressing cancers, though current inhibitors are sub-optimal due in part to poor physical properties. We are pursuing heterocyclic MCT1 inhibitors in novel scaffolds for evaluation. Here we report a synthetic route for a library of pteridine diones, their potency against MCT1-expressing human Raji Burkitt lymphoma cells using MTT assays, and the structure-activity relationships for this structural class.

Synthesis of pteridine diones as potential monocarboxylate transporter 1 (MCT1) inhibitors

250th National Meeting (2015)

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