Synthesis and antitumor activity of novel C-7 paclitaxel ethers: discovery of BMS-184476
T J Altstadt1, C R Fairchild, J Golik
1Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, P.O. Box 5100, Wallingford, Connecticut 06492-7660, USA.
Journal of Medicinal Chemistry
|December 14, 2001
Abstract:
The preparation of C-7 paclitaxel ethers is described. Various substituted ethers were prepared via activation of the corresponding methylthiomethyl ether followed by alcohol addition. Variation of the C-7 ether group as well the 3' side chain position led to the discovery of a novel taxane, BMS-184476 (4), with preclinical antitumor activity superior to paclitaxel.


