Abstract
The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.
MeSH terms
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Animals
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Cell Cycle
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Cell Cycle Proteins / antagonists & inhibitors*
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Cell Cycle Proteins / chemistry
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Cell Line, Tumor
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Cell Proliferation
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Mice
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Mitosis
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Models, Chemical
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Molecular Conformation
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Polo-Like Kinase 1
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Protein Serine-Threonine Kinases / chemistry
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Proto-Oncogene Proteins / antagonists & inhibitors*
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Proto-Oncogene Proteins / chemistry
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Thiophenes / antagonists & inhibitors*
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Thiophenes / chemistry
Substances
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Cell Cycle Proteins
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Enzyme Inhibitors
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Proto-Oncogene Proteins
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Thiophenes
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Protein Serine-Threonine Kinases