Abstract
A series of 3-nitrochromenes were designed and synthesized. These compounds showed good inhibitory activity against thioredoxin reductase (TrxR) and the proliferation of A549 cancer cells. The structure-activity relationship analysis indicates that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. The bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Benzopyrans / chemical synthesis
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Benzopyrans / chemistry
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Benzopyrans / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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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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Humans
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Nitro Compounds / chemical synthesis
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Nitro Compounds / chemistry
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Nitro Compounds / pharmacology*
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Structure-Activity Relationship
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Thioredoxin-Disulfide Reductase / antagonists & inhibitors*
Substances
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Benzopyrans
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Enzyme Inhibitors
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Nitro Compounds
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Thioredoxin-Disulfide Reductase