Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).

@article{Brooke2014TargetingTW,
  title={Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).},
  author={Darby G Brooke and Ellen M van Dam and Colin K. W. Watts and Amanda El Khoury and Marie A. Dziadek and Harold F. Brooks and Lisa-Jane K Graham and Jack Urquhart Flanagan and William A. Denny},
  journal={Bioorganic & medicinal chemistry},
  year={2014},
  volume={22 3},
  pages={
          1029-39
        }
}
High-throughput screening of a small-molecule library identified a 5-triazolo-2-arylpyridazinone as a novel inhibitor of the important glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Such inhibitors are of interest due to PFKFB3's control of the important glycolytic pathway used by cancer cells to generate ATP. A series of analogues was synthesized to study structure-activity relationships key to enzyme inhibition. Changes to the triazolo or pyridazinone rings were not… CONTINUE READING
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