Triple negative breast cancer (TNBC) constitutes 10–20% of all breast cancers and is associated with aggressive tumor growth, recurrence, metastasis and poor patient outcome. TNBC adopts vigorous glycolysis to meet the increased energy demand of the tumor. Lactic acid is then generated as the main energy source.   Export of this lactic acid out of the cell is essential to prevent a decrease in intracellular pH and avoid apoptosis.  Lactic acid influx and efflux from cells is facilitated by members of the mono-carboxylate transporter family known as MCT1 and MCT4. Potent dual MCT 1 & 4 inhibitors have been developed based on α-cyano-4-hydroxy cinnamic acid template. Utilizing this template we were able to complete an extensive <i>in vitro </i>based SAR. These studies were then followed by xenografts on MDA-MB-231 which showed our MCT inhibitors have the potential to act as single agent anti-cancer agents as well as in combination with standard chemotherapy to realize their synergistic potential.<br/><br/>

Potent dual monocarboxylate transporter 1 & 4 inhibitors for triple negative breast cancer treatment

249th National Meeting (2015)

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