Abstract
High-throughput screening has resulted in the discovery of thiosemicarbazone thrombopoietin mimics. A shared pharmacophore hypothesis between this series and a previously identified class, the pyrazol-4-ylidenehydrazines, led to the rapid optimization of both potency and efficacy of the thiosemicarbazones. The application of high-throughput chemistry and purification techniques allowed for the rapid elucidation of structure-activity relationships.
MeSH terms
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Aldehydes / chemical synthesis*
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Aldehydes / chemistry
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Aldehydes / pharmacology
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Cell Division / drug effects
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Cell Line
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Combinatorial Chemistry Techniques
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Humans
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Models, Molecular
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Molecular Mimicry
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Phosphorylation
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Recombinant Proteins / pharmacology
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Structure-Activity Relationship
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Thiosemicarbazones / chemical synthesis*
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Thiosemicarbazones / chemistry
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Thiosemicarbazones / pharmacology
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Thrombopoietin / chemistry*
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Thrombopoietin / pharmacology
Substances
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Aldehydes
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Recombinant Proteins
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Thiosemicarbazones
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salicylaldehyde thiosemicarbazone
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Thrombopoietin