Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk)

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3152-8. doi: 10.1016/j.bmcl.2011.02.114.
Andrew S Rosenthal  1 ,  Cordelle Tanega ,  Min Shen ,  Bryan T Mott ,  James M Bougie ,  Dac-Trung Nguyen ,  Tom Misteli ,  Douglas S Auld ,  David J Maloney ,  Craig J Thomas
Affiliations
  • 1. NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.
PMID: 21450467 DOI: 10.1016/j.bmcl.2011.02.114
Abstract

Continued examination of substituted 6-arylquinazolin-4-amines as CLK4 inhibitors resulted in selective inhibitors of CLK1, CLK4, DYRK1A and DYRK1B. Several of the most potent inhibitors were validated as being highly selective within a comprehensive kinome scan.