Abstract
Various kinds of water-soluble 9-acyloxyellipticine derivatives were synthesized in a search for compounds with potent antitumor activity. Antitumor activities against several tumors in mice (P388 leukemia, colon 26, Lewis lung carcinoma and B16 melanoma) were evaluated by using intravenous administration. Many compounds exhibited good antitumor activities; in particular, the glutarate derivative (5o) showed potent antitumor activity. This compound (5o) may be converted to 9-hydroxyellipticine (2) by enzyme-catalyzed hydrolysis in the body.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Carcinoma, Lewis Lung / drug therapy
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Carcinoma, Lewis Lung / metabolism
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Colonic Neoplasms / drug therapy
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Colonic Neoplasms / metabolism
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Drug Screening Assays, Antitumor
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Ellipticines / chemical synthesis*
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Ellipticines / pharmacokinetics
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Ellipticines / pharmacology*
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Leukemia P388 / drug therapy
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Leukemia P388 / metabolism
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Lung Neoplasms / drug therapy
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Lung Neoplasms / metabolism
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Male
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Melanoma, Experimental / drug therapy
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Melanoma, Experimental / metabolism
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Mice
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Mice, Inbred Strains
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Structure-Activity Relationship
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Tissue Distribution
Substances
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Antineoplastic Agents
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Ellipticines