Abstract
'Bended' 1, 3 or 'linear' 2 pyrrolidino-fused (aza)carbazoles were prepared and screened towards a few cancer-related targets. Whereas 'bended' derivatives 1 and 3 proved to be weakly toxic, several members of the 'linear' family strongly interact with DNA, especially derivative 28a.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / toxicity
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CDC2 Protein Kinase / antagonists & inhibitors
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CDC2 Protein Kinase / metabolism
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Carbazoles / chemical synthesis
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Carbazoles / chemistry*
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Carbazoles / pharmacology*
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Carbazoles / toxicity
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Carbolines / chemical synthesis
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Carbolines / chemistry*
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Carbolines / pharmacology*
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Carbolines / toxicity
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Cell Cycle / drug effects
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Cell Line, Tumor
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DNA / genetics
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DNA / metabolism
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DNA Footprinting
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DNA Topoisomerases, Type I / metabolism
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Enzyme Inhibitors / toxicity
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Glycogen Synthase Kinase 3 / antagonists & inhibitors
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Glycogen Synthase Kinase 3 / metabolism
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Glycogen Synthase Kinase 3 beta
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Indoles / chemistry
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Inhibitory Concentration 50
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Mice
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Molecular Structure
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Nucleic Acid Denaturation
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Pyrroles / chemistry*
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Structure-Activity Relationship
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Temperature
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Titrimetry
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Topoisomerase I Inhibitors
Substances
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Antineoplastic Agents
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Carbazoles
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Carbolines
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Enzyme Inhibitors
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Indoles
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Pyrroles
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Topoisomerase I Inhibitors
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indole
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DNA
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Glycogen Synthase Kinase 3 beta
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CDC2 Protein Kinase
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Glycogen Synthase Kinase 3
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glycogen synthase kinase 3 alpha
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DNA Topoisomerases, Type I