Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 12, Pages 3654-3661Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.096
Keywords
Clk; Dyrk; Kinase inhibitor; Splicing; Pyrimidine
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Funding
- National Institutes of Health [U54 HG005031, RO3 MH084827-01, U54 MH084681-01]
- Division of Preclinical Innovation, National Center for Advancing Translational Sciences of the National Institutes of Health
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Substituted pyrimidine inhibitors of the Clk and Dyrk kinases have been developed, exploring structure-activity relationships around four different chemotypes. The most potent compounds have low-nanomolar inhibitory activity against Clk1, Clk2, Clk4, Dyrk1A and Dyrk1B. Kinome scans with 442 kinases using agents representing three of the chemotypes show these inhibitors to be highly selective for the Clk and Dyrk families. Further off-target pharmacological evaluation with ML315, the most selective agent, supports this conclusion. (C) 2013 Elsevier Ltd. All rights reserved.
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