Abstract
Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.
MeSH terms
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Humans
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MAP Kinase Kinase Kinases / antagonists & inhibitors*
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Models, Molecular*
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Molecular Conformation
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Molecular Structure
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Proto-Oncogene Proteins / antagonists & inhibitors*
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology*
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Structure-Activity Relationship
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Thiophenes / chemical synthesis*
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Thiophenes / chemistry
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Thiophenes / pharmacology*
Substances
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Proto-Oncogene Proteins
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Pyridines
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Thiophenes
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MAP Kinase Kinase Kinases
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MAP3K8 protein, human