Abstract
A series of prodrugs of 4'-demethyl-4-deoxypodophyllotoxin (DDPT) including carbamates (3-8), a carbonate (9) and water-soluble amino acid derivatives (10-17) were prepared and tested for their antitumor activity. The carbamate 6 (2-hydroxyethylcarbamoyl-DDPT), carbonate 9 (2-chloroethyloxycarbonyl-DDPT), and most of amino acid prodrugs (12-17) showed enhanced antitumor activity.
MeSH terms
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Amino Acids / chemistry
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Carbamates / chemistry
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Carbonates / chemistry
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Drug Screening Assays, Antitumor
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Drugs, Chinese Herbal
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Humans
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Hydrolysis
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Lethal Dose 50
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Podophyllotoxin / analogs & derivatives*
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Podophyllotoxin / chemistry*
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Podophyllotoxin / pharmacology*
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Prodrugs / chemical synthesis*
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Prodrugs / pharmacology*
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Amino Acids
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Antineoplastic Agents
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Carbamates
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Carbonates
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Drugs, Chinese Herbal
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Prodrugs
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deoxypodophyllotoxin
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Podophyllotoxin