Synthesis of taxoids with improved cytotoxicity and solubility for use in tumor-specific delivery

…, E Baloglu, VS Goldmacher, RVJ Chari

Index: Miller, Michael L.; Roller, Elizabeth E.; Zhao, Robert Y.; Leece, Barbara A.; Ab, Olga; Baloglu, Erkan; Goldmacher, Victor S.; Chari, Ravi V. J. Journal of Medicinal Chemistry, 2004 , vol. 47, # 20 p. 4802 - 4805

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Citation Number: 28

Abstract

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 ...