Advanced cancer patients experience aggressive tumor proliferation and metastasis. These tumors require increased energy demands and adopt vigorous glycolysis to support their demands. As a result of glycolysis the cells produce excess lactic acid inside the cell. Mono-carboxylate transports 1 and 4 (MCT 1 and 4) have the responsibility of influx/efflux of the lactate. Inhibition of MCT 1 and/or 4 is thought to decrease cellular pH and cause cellular toxicity. Recently, we have synthesized novel coumarin based small molecules that have the ability to inhibit these transporters. Here we present the synthesis of these new novel derivatives as well as toxicity results from several human and murine cell lines. We also present some of anticancer efficacy studies in vivo.

Novel coumarin based monocarboxylate transport 1 & 4 inhibitors as anticancer agents

249th National Meeting (2015)

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