A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors.

@article{MartnAcosta2018ANF,
  title={A new family of densely functionalized fused-benzoquinones as potent human protein kinase CK2 inhibitors.},
  author={Pedro Mart{\'i}n-Acosta and S. Haider and {\'A}ngel Amesty and D. Aichele and J. Jose and A. Est{\'e}vez-Braun},
  journal={European journal of medicinal chemistry},
  year={2018},
  volume={144},
  pages={
          410-423
        }
}
A new series of 2-amino-4-phenyl-6-hydroxy-7-alkyl-pyranobenzoquinones was synthesized as ATP-competitive CK2 inhibitors. They were readily synthesized through a three-component Knoevenagel condensation-Michael addition-heterocyclization reaction from aldehydes, malononitrile, and 3-alkyl-2,5-dihydroxybenzoquinones. Some of the synthesized compounds presented interesting inhibitory activity with IC50 values in the submicromolar range. A structure-activity relationship study was carried out and… Expand
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