Abstract
We synthesized novel water-soluble and orally active taxane analogues, 7-deoxy-9beta-dihydro-9,10-O-acetal taxanes. Cytotoxicities of the synthetic compounds were greater than those of paclitaxel and docetaxel, especially against resistant cancer cell lines expressing P-glycoprotein. In addition, some compounds showed potent antitumor effects against B16 melanoma BL6 in vivo by both iv and po administration.
MeSH terms
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Animals
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Antineoplastic Agents, Phytogenic / chemical synthesis*
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / pharmacology
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Cell Survival / drug effects
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Crystallography, X-Ray
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Drug Screening Assays, Antitumor
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Humans
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Indicators and Reagents
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Melanoma, Experimental / drug therapy
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Mice
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Molecular Conformation
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Neoplasm Transplantation
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Paclitaxel / analogs & derivatives*
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Paclitaxel / chemical synthesis*
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Paclitaxel / pharmacology
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Solubility
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents, Phytogenic
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Indicators and Reagents
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Paclitaxel