Abstract
Diversely substituted 2-pyrrolines have been prepared by a novel multicomponent process involving a reaction of various N-(aryl- and alkylsulfonamido)-acetophenones with aldehydes and malononitrile. While the reaction is highly regioselective, it is not stereoselective, generating a mixture of cis and trans 2-pyrrolines. A number of analogs from both cis and trans 2-pyrroline libraries were found to have antiproliferative activity in human cancer cell lines.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Acetophenones / chemistry
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Aldehydes / chemistry
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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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Apoptosis / drug effects
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Cell Growth Processes / drug effects
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Cell Line, Tumor
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Crystallography, X-Ray
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Isomerism
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Jurkat Cells
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Nitriles / chemistry
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Structure-Activity Relationship
Substances
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Acetophenones
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Aldehydes
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Antineoplastic Agents
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Nitriles
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Pyrroles
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pyrroline
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dicyanmethane