To develop effective taxane-antibody immunoconjugates, we have prepared a series of modified taxanes that have both improved toxicity and solubility in aqueous systems as compared to paclitaxel (1a). These taxanes have been modified at either the C-10 or C-7 position and were found to be very cytotoxic against both normal and multi-drug-resistant (MDR) cells, as well as up to 30 times more soluble than paclitaxel in various buffer systems.
Terpenes U 0200 Synthesis and Biological Evaluation of Novel Taxoids Designed for Targeted Delivery to Tumors. -Twenty-three new taxoids of type (I) with significantly higher cytotoxicity than paclitaxel or docetaxel are presented. -(BALOGLU*, E.; MILLER, M. L.; ROLLER, E. E.; CAVANAGH, E. E.; LEECE, B. A.; GOLDMACHER, V. S.; CHARI, R. V.
Abstrac: A one-pot synthesis of 7-triethylsilylbaccatin III has been delineated. The reaction can easily be extended for the preparation of analogs of baccatin III.
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