Abstract
9-Trifluoromethyl-paullones with a carbon chain in the 2-position were synthesized by palladium-catalyzed coupling reactions of a 2-iodoprecursor with terminal alkenes or alkynes, respectively. The introduction of a 2-cyanoethyl substituent led to a significant enhancement of CDK1/cyclin B inhibiting property and in vitro antiproliferative activity.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Benzazepines / chemical synthesis*
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Benzazepines / pharmacology
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CDC2 Protein Kinase / antagonists & inhibitors*
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Cell Division / drug effects
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Histones / metabolism
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Humans
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Oocytes / drug effects
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Oocytes / enzymology
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Starfish
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Benzazepines
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Enzyme Inhibitors
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Histones
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Indoles
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CDC2 Protein Kinase