Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 13, Pages 4420-4424Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.05.017
Keywords
Meridianins; Suzuki cross-coupling; Kinase inhibitors; Dyrk1A inhibitors
Funding
- 'Association France-Alzheimer Finistere (LM)
- CRITT Sante Bretagne (LM)
- 'Fondation Jerome Lejeune' (LM)
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The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1 delta/epsilon, GSK-3 alpha/beta, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1). (C) 2009 Elsevier Ltd. All rights reserved.
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