Abstract
A series of novel podophyllotoxin (PDT) analogues was synthesized in which the lactone moiety was shifted to C ring. Some of the derivatives were also synthesized with modified A ring. Analogues 23 and 25 exhibited potent in vitro cytotoxicity against colon cancer (CaCO(2)) cell line. p-Demethylated E-ring analogues exhibited better potency than the corresponding methylated analogues. These analogues showed toxicity comparable to PDT against human erythrocytes albeit at much higher concentrations (100 microg/ml) than their cytotoxicity values.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Cell Line, Tumor
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Cell Survival / drug effects
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Erythrocytes / drug effects
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Hemolysis / drug effects
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Humans
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Lactams / chemistry*
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Lactones / chemistry*
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Molecular Structure
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Neoplasms / drug therapy*
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Podophyllotoxin / analogs & derivatives*
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Podophyllotoxin / chemical synthesis
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Podophyllotoxin / pharmacology*
Substances
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Antineoplastic Agents
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Lactams
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Lactones
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Podophyllotoxin