Abstract
7-Deoxypaclitaxel, 10-deacetoxypaclitaxel and 10-deacetoxy-7-deoxypaclitaxel were prepared and evaluated for their ability to promote assembly of tubulin into microtubules, their cytotoxicity against NCI/ADR-RES cells and for their interactions with P-glycoprotein in bovine brain microvessel endothelial cells. The three compounds were essentially equivalent to paclitaxel in cytotoxicity against NCI/ADR-RES cells. They also appeared to interact with P-glycoprotein in the endothelial cells with the two 10-deacetoxy compounds having less interaction than paclitaxel and 7-deoxypaclitaxel.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Brain / blood supply*
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Brain / cytology
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Brain / drug effects
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Cattle
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Cell Line, Tumor
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Cell Survival / drug effects
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Drug Screening Assays, Antitumor
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Endothelial Cells / drug effects*
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Humans
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Molecular Conformation
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Neoplasms, Experimental / drug therapy*
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Paclitaxel / analogs & derivatives*
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Paclitaxel / chemical synthesis
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Paclitaxel / chemistry
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Paclitaxel / pharmacology
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Structure-Activity Relationship
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Taxoids / chemical synthesis
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Taxoids / chemistry
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Taxoids / pharmacology
Substances
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10-deacetoxy-7-deoxypaclitaxel
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10-deacetoxypaclitaxel
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7-deoxypaclitaxel
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Taxoids
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Paclitaxel