Inhibition of mitochondrial complex I (NADH:ubiquinone oxidoreductase) has been shown to negatively affect proliferative tissue undergoing aerobic glycolysis due to the Warburg effect. The potential implications in cancer therapeutics led us to develop a diverse class of novel benzhydrol complex I inhibitors. Many of these analogues inhibit mitochondrial complex I as well as the hypoxia inducible factor 1 (HIF-1) pathway, an important transcription factor for cell survival in low oxygen concentrations. We will present qualitative and quantitative structure-activity relationships that may provide some insights into future direction for establishing new analogues as well as to establish the proposed mode of <i>in vivo</i> cancer treatment.

Novel mitochondrial complex I inhibitors for anti-cancer therapeutics

253rd National Meeting (2017)

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