Abstract
The synthesis and biological evaluation of libraries of 8-biarylchromen-4-ones enabled the elucidation of structure-activity relationships for inhibition of the DNA-dependent protein kinase (DNA-PK), with 8-(3-(thiophen-2-yl)phenyl)chromen-4-one and 8-(3-(thiophen-3-yl)phenyl)chromen-4-one being especially potent inhibitors.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Chromones / chemical synthesis
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Chromones / chemistry*
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Chromones / pharmacology*
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DNA-Activated Protein Kinase / antagonists & inhibitors*
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HeLa Cells
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Humans
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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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Radiation-Sensitizing Agents / chemical synthesis
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Radiation-Sensitizing Agents / chemistry
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Radiation-Sensitizing Agents / pharmacology
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Structure-Activity Relationship
Substances
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Chromones
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Protein Kinase Inhibitors
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Radiation-Sensitizing Agents
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DNA-Activated Protein Kinase