Abstract
A series of thieno[3,2-b]pyrroloazepinones derivatives related to Hymenialdisine were prepared and tested for CHK1 inhibitory activity. Nanomolar inhibitions were achieved when electron-withdrawing substituents were introduced at position 3 of the thiophene ring.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Azepines / chemical synthesis*
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Azepines / pharmacology
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Checkpoint Kinase 1
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Screening Assays, Antitumor
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Electrons
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Neoplasms / drug therapy
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Protein Kinases / metabolism*
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology
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Structure-Activity Relationship
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Thiophenes / chemistry
Substances
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Antineoplastic Agents
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Azepines
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Pyrroles
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Thiophenes
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hymenialdisine
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Protein Kinases
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CHEK1 protein, human
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Checkpoint Kinase 1