Discovery of benzo[e]pyridoindolones as kinase inhibitors that disrupt mitosis exit while erasing AMPK-Thr172 phosphorylation on the spindle

@inproceedings{Le2015DiscoveryOB,
  title={Discovery of benzo[e]pyridoindolones as kinase inhibitors that disrupt mitosis exit while erasing AMPK-Thr172 phosphorylation on the spindle},
  author={Ly-Thuy-Tram Le and Morgane Couvet and Bertrand Favier and Jean-Luc Coll and C Nguyen and Annie Molla},
  booktitle={Oncotarget},
  year={2015}
}
Aurora kinases play an essential role in mitotic progression and are attractive targets in cancer therapy. The first generation of benzo[e]pyridoindole exhibited powerful aurora kinase inhibition but their low solubility limited further development. Grafting a pyperidine-ethoxy group gives rise to a hydrosoluble inhibitor: compound C5M.C5M could efficiently… CONTINUE READING