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Bioorg Med Chem Lett. 2009 Dec 1;19(23):6700-5. doi: 10.1016/j.bmcl.2009.09.121. Epub 2009 Oct 3.

Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).

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1
NIH Chemical Genomics Center, National Human Genome Research Institute, Bethesda, MD 20892-3370, USA.

Abstract

A series of substituted 6-arylquinazolin-4-amines were prepared and analyzed as inhibitors of Clk4. Synthesis, structure-activity relationships and the selectivity of a potent analogue against a panel of 402 kinases are presented. Inhibition of Clk4 by these agents at varied concentrations of assay substrates (ATP and receptor peptide) highly suggests that this chemotype is an ATP competitive inhibitor. Molecular docking provides further evidence that inhibition is the result of binding at the kinase hinge region. Selected compounds represent novel tools capable of potent and selective inhibition of Clk1, Clk4, and Dyrk1A.

PMID:
19837585
PMCID:
PMC2807730
DOI:
10.1016/j.bmcl.2009.09.121
[Indexed for MEDLINE]
Free PMC Article
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