Abstract
The evolution of 2, a C-4-methylcarbonate analogue of paclitaxel with minimal oral bioavailability and oral efficacy, into its C-3'-t-butyl-3'-N-t-butyloxycarbonyl analogue (15i), a novel taxane with oral efficacy in preclinical models that is comparable to iv administered paclitaxel, is described.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Biological Availability
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Bridged-Ring Compounds / chemistry
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Bridged-Ring Compounds / pharmacokinetics*
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Bridged-Ring Compounds / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Drug Evaluation, Preclinical
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Humans
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Inhibitory Concentration 50
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Mice
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Rats
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Structure-Activity Relationship
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Taxoids / chemistry
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Taxoids / pharmacokinetics*
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Taxoids / pharmacology
Substances
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Antineoplastic Agents
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BMS-275183
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Bridged-Ring Compounds
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Taxoids
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taxane