Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.

@article{Mariano2016SystematicDO,
  title={Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.},
  author={Marica Mariano and Rolf W. Hartmann and Matthias Engel},
  journal={European journal of medicinal chemistry},
  year={2016},
  volume={112},
  pages={209-216}
}
The dual-specificity tyrosine-regulated kinase 1A (Dyrk1A) has gathered much interest as a pharmacological target in Alzheimer's disease (AD), but it plays a role in malignant brain tumors as well. As both diseases are multi-factorial, further protein kinases, such as Clk1 and CK2, were proposed to contribute to the pathogenesis. We designed a new class of… CONTINUE READING