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外文会议>the European Peptide Symposium
>APPLICATION OF O-N INTRAMOLECULAR CARBONATE-CARBAMATE MIGRATION: MIGRATION OF PROTECTIVE GROUPS IN AMINO ACIDS AND WATER-SOLUBLE PRODRUG STRATEGY
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APPLICATION OF O-N INTRAMOLECULAR CARBONATE-CARBAMATE MIGRATION: MIGRATION OF PROTECTIVE GROUPS IN AMINO ACIDS AND WATER-SOLUBLE PRODRUG STRATEGY
The introduction of anti-cancer agents, paclitaxel (Taxol) and docetaxel (Taxotere), has revolutionized the treatment of cancer. Moreover, other taxoids have been recently developed with improved antitumor potency. However, despite the promise that these agents have engendered, their poor water-solubility is a serious problem in intravenous administration. To overcome this problem we have developed new prodrug strategy based on, a well-known reaction in peptide chemistry, O-N intramolecular acyl migration. Prodrugs of paclitaxel and other taxoids, 2'-O-acyl isoforms of parent drugs, showed higher water-solubility and promising kinetics data.
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