Abstract
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.
MeSH terms
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Aurora Kinases
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Benzothiazoles / chemistry*
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Benzothiazoles / pharmacology*
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Cell Line, Tumor
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ErbB Receptors / chemistry
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ErbB Receptors / metabolism
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Humans
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Models, Molecular
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Molecular Structure
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Phosphorylation / drug effects
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Protein Binding
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology*
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Protein Kinases / chemistry
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Protein Kinases / metabolism*
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Protein Serine-Threonine Kinases / chemistry
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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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Benzothiazoles
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Protein Kinase Inhibitors
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Protein Kinases
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ErbB Receptors
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Aurora Kinases
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Protein Serine-Threonine Kinases
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benzothiazole