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

Journal of Medicinal Chemistry
Michael L MillerRavi V J Chari

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 systems.

References

Mar 21, 2002·The Lancet Oncology·Brian Leyland-Jones
Dec 13, 2002·Journal of Medicinal Chemistry·Iwao OjimaRavi V J Chari

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Citations

Aug 21, 2007·Accounts of Chemical Research·Ravi V J Chari
Sep 30, 2005·Natural Product Reports·James R Hanson
Mar 1, 2011·Therapeutic Delivery·Victor S Goldmacher, Yelena V Kovtun
Jul 29, 2009·Chemical Biology & Drug Design·Rajeshwar P Verma, Corwin Hansch
Nov 14, 2006·Analytical Biochemistry·Shubhada SharmaSusan Bane
Dec 11, 2013·Organic & Biomolecular Chemistry·Hendra WahyudiShelli R McAlpine
Sep 17, 2013·Chemical Communications : Chem Comm·Peng AnQing Lin
Jun 1, 2021·Bioorganic & Medicinal Chemistry·Sumei RenNing Ding
Oct 31, 2013·Journal of the American Chemical Society·Zhipeng YuQing Lin

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