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Synthesis and Biological Evaluation of 1-Deoxypaclitaxel Analogues
David G. I. Kingston1, Mahendra D. Chordia, Prakash G. Jagtap
1Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, New Jersey 05843.
The Journal of Organic Chemistry
|October 25, 2001
Abstract:
The naturally occurring taxoid baccatin VI has been converted to various 1-deoxypaclitaxel derivatives by selective deacylation followed by attachment of the C-13 side chain. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with activity comparable to that of paclitaxel were discovered. It thus appears that the 1-hydroxyl group is not necessary for the activity of paclitaxel.