Abstract
To investigate structure-activity relationships of the 9,10-acetal-9beta-dihydro taxoids, we modified the 7-hydroxyl groups of the 9,10-acetonide-3'-(4-pyridyl) analogue to deoxy, methoxy, alpha-F, and 7beta,8beta-methano group. As a result of this study, we found that the 7-deoxy analogue was the strongest among these analogues. In addition, we found that the 7-deoxy-3'-(4-pyridyl) and 7-deoxy-3'-(2-pyridyl) analogues showed stronger activity against cell lines expressing P-glycoprotein than the corresponding 3'-phenyl analogue.
MeSH terms
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Antineoplastic Agents, Phytogenic / chemical synthesis*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Bridged-Ring Compounds / chemistry
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Chemical Phenomena
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Chemistry, Physical
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Chromatography, High Pressure Liquid
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Drug Screening Assays, Antitumor
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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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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Stereoisomerism
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Structure-Activity Relationship
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Taxoids*
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents, Phytogenic
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Bridged-Ring Compounds
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Indicators and Reagents
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Taxoids
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taxane
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Paclitaxel