Abstract
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, CK1delta/epsilon, GSK-3alpha/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).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Cells, Cultured
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Fibroblasts / cytology
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Humans
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Indole Alkaloids / chemical synthesis*
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Indole Alkaloids / chemistry
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Indole Alkaloids / pharmacology*
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Protein Kinases / metabolism*
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Rats
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Structure-Activity Relationship
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Swine
Substances
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Indole Alkaloids
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Protein Kinase Inhibitors
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Protein Kinases