Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 15, Pages 4592-4596Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.103
Keywords
Anaplastic lymphoma kinase (ALK); Kinase inhibitor; Small library synthesis
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Funding
- American Lebanese Syrian Associated Charities (ALSAC), St. Jude Children's Research Hospital
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We report the synthesis of a pyrimidinone library that targets anaplastic lymphoma kinase (ALK), an oncogenic receptor tyrosine kinase. This library was generated in three steps from a versatile commercially available starting material. Some compounds within this library showed single digit micromolar inhibition of ALK in vitro, while showing minimal inhibition of other homologous insulin receptor family kinases including the human insulin receptor kinase (IRK), at the highest concentrations investigated. We also present initial ALK structure-activity relationships for this library. (C) 2011 Elsevier Ltd. All rights reserved.
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