Williams, Michael2019-06-122019-06-122017-04https://hdl.handle.net/11299/203563University of Minnesota M.S. thesis. 2017. Major: Chemistry. Advisor: Venkatram Mereddy. 1 computer file (PDF); 146 pages.Cancer cells pursue aggressive glycolysis for ATP generation and rapid cell proliferation. Disruption of glycolysis leads to tumor growth inhibition and hence glycolytic inhibitors can be developed as anticancer agents. Monocarboxylate transporters 1 and 4 are involved in the efflux and influx of glycolytic end products lactate and pyruvate in cancer cells and inhibition of these transporters is a novel way to arrest the tumor growth. In the present work, several α,β-unsaturated imidazolidine diones have been synthesized as potential MCT1 inhibitors that can cross the blood brain barrier. Unfortunately, none of the compounds exhibit any MCT1 inhibition properties even at high concentrations. In another project, α-cyanoacyloxyamides from α-cyanocinnamic acid and 4-hydroxy-α-cyanocinnamic acid (CHC) have been synthesized via three component Passerini reaction. The preliminary biological studies indicate that several of Passerini based prodrugs exhibit moderate to good MCT1 inhibition properties at low µM concentration. Importantly, some of these prodrugs exhibit 100-200 times more potency than the parent CHC molecule. Future studies should involve more biological studies to identify a lead candidate compound for further development.enThesis or Dissertation