Abstract
A series of palmarumycin prodrugs and water-soluble analogs has been synthesized and assayed for inhibition of the thioredoxin-thioredoxin reductase system. Increased aqueous solubility led to an improved in vivo activity profile.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Humans
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Prodrugs / chemical synthesis*
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Prodrugs / pharmacology
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Solubility
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacology
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Structure-Activity Relationship
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Thioredoxin-Disulfide Reductase / antagonists & inhibitors*
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Thioredoxins / antagonists & inhibitors
Substances
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Antineoplastic Agents
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Naphthalenes
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Prodrugs
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Spiro Compounds
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palmarumycin C2
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Thioredoxins
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Thioredoxin-Disulfide Reductase