Abstract
A general route to ruthenium pyridocarbazole half-sandwich complexes is presented and applied to the synthesis of sixteen new compounds, many of which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into the pyridine moiety increases the binding affinity for glycogen synthase kinase 3 by almost one order of magnitude. These data are supplemented with cyclic voltammetry experiments and a protein co-crystallographic study.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Carbazoles / chemical synthesis
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Carbazoles / chemistry
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Carbazoles / pharmacology*
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Crystallography, X-Ray
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Ligands
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Models, Molecular
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Molecular Structure
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Organometallic Compounds / chemical synthesis
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Organometallic Compounds / chemistry
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Organometallic Compounds / 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 / drug effects*
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Ruthenium / chemistry*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Carbazoles
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Ligands
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Organometallic Compounds
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Protein Kinase Inhibitors
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Ruthenium
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Protein Kinases