Abstract
A series of substituted benzo[c][2,7]-naphthyridines were prepared and showed good potency in inhibiting PDK-1. The synthesis and SAR of this series of compounds are presented as well as the X-ray crystal structure of one of these analogs in a complex with PDK-1.
MeSH terms
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3-Phosphoinositide-Dependent Protein Kinases
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Binding Sites
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Crystallography, X-Ray
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Humans
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Molecular Conformation
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Naphthyridines / chemical synthesis
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Naphthyridines / chemistry*
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Naphthyridines / 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 Serine-Threonine Kinases / antagonists & inhibitors*
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Protein Serine-Threonine Kinases / metabolism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Naphthyridines
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Protein Kinase Inhibitors
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3-Phosphoinositide-Dependent Protein Kinases
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Protein Serine-Threonine Kinases