Abstract
Analysis of the methanolic extract of Calotropis procera root barks enabled the identification of a novel cardenolide (2''-oxovoruscharin) to be made. Of the 27 compounds that we hemisynthesized, one (23) exhibited a very interesting profile with respect to its hemisynthetic chemical yield, its in vitro antitumor activity, its in vitro inhibitory influence on the Na+/K+-ATPase activity, and its in vivo tolerance. Compound 23 displayed in vitro antitumor activity on a panel of 57 human cancer cell lines similar to taxol, and higher than SN-38 (the active metabolite of irinotecan), two of the most potent drugs used in hospitals to combat cancer.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / pharmacology
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Calotropis / chemistry*
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Camptothecin / analogs & derivatives*
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Camptothecin / pharmacology
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Cardenolides / chemical synthesis*
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Cardenolides / isolation & purification*
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Cardenolides / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cerebral Cortex / chemistry
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Drug Resistance, Multiple
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor
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Etoposide / pharmacology
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Humans
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Irinotecan
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Magnetic Resonance Spectroscopy
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Maximum Tolerated Dose
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Mice
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Organoplatinum Compounds / pharmacology
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Oxaliplatin
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Paclitaxel / pharmacology
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Sodium-Potassium-Exchanging ATPase / chemistry
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Structure-Activity Relationship
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Swine
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Thiazoles / chemical synthesis*
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Thiazoles / isolation & purification*
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Thiazoles / pharmacology
Substances
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2''-oxovoruscharin
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Antineoplastic Agents
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Cardenolides
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Organoplatinum Compounds
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Thiazoles
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Oxaliplatin
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Etoposide
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Irinotecan
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Sodium-Potassium-Exchanging ATPase
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Paclitaxel
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Camptothecin