It is well-known that cancer cells gain energy through a high rate of glycolysis, even under conditions of sufficient oxygen. Lactate, the end product of glycolysis, must be effluxed by monocarboxylate transporters (MCTs) to maintain intracellular pH levels. Four such transporters, MCT1-4, are known, and the isoforms MCT1 and MCT4 are predominantly responsible for lactate transportation in tumor cells.   Thus inhibitors of MCT1 and/or MCT4 are potential therapeutic agents for treatment of cancers. We herein report our efforts toward the development of MCT1 inhibitors in three novel scaffolds: pteridines, xanthines, and flavonoids.  We will discuss their synthesis and SAR studies to optimize antitumor effects in cell-based assays.

Exploration of novel scaffolds for MCT1 inhibition: New antitumor agents

247th National Meeting (2014)

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