Abstract
Imidazo[1,2-a]pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Cell Line, Tumor
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Dose-Response Relationship, Drug
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Drug Design*
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High-Throughput Screening Assays
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MAP Kinase Kinase Kinase 5 / antagonists & inhibitors*
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MAP Kinase Kinase Kinase 5 / metabolism
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Models, Molecular
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Molecular Structure
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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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Pyridines / chemical synthesis
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Pyridines / chemistry
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Pyridines / pharmacology*
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Rats
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Structure-Activity Relationship
Substances
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Protein Kinase Inhibitors
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Pyridines
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MAP Kinase Kinase Kinase 5
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imidazo(1,2-a)pyridine