Abstract
The syntheses of a series of dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted in 10-position with saturated and unsaturated side chains, via palladium catalyzed cross-coupling reactions, are described. These compounds can be considered as granulatimide bis-imide analogues. Their inhibitory activity toward Chk1 kinase and their antiproliferative activities in vitro in four tumor cell lines are reported.
MeSH terms
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Animals
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Carbazoles / chemical synthesis*
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Carbazoles / pharmacology*
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Catalysis
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Checkpoint Kinase 1
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Cyclization
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Drug Screening Assays, Antitumor
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Humans
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In Vitro Techniques
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Molecular Structure
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Palladium / chemistry*
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Protein Kinases / drug effects
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Carbazoles
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Pyrroles
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dipyrrolo(3,4-a:3,4-c)carbazole-1,3,4,6-tetraone
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Palladium
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Protein Kinases
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CHEK1 protein, human
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Checkpoint Kinase 1