title: Synthesis and Biological Evaluation of 1-Deoxypaclitaxel Analogues.
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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 4000, Princeton, New Jersey 05843.
authors.forename: David G. I.
authors.initials: DG
authors.lastname: Kingston
authors.forename: Mahendra D.
authors.initials: MD
authors.lastname: Chordia
authors.forename: Prakash G.
authors.initials: PG
authors.lastname: Jagtap
authors.forename: Jingyu
authors.initials: J
authors.lastname: Liang
authors.forename: Ya-Ching
authors.initials: YC
authors.lastname: Shen
authors.forename: Byron H.
authors.initials: BH
authors.lastname: Long
authors.forename: Craig R.
authors.initials: CR
authors.lastname: Fairchild
authors.forename: Kathy A.
authors.initials: KA
authors.lastname: Johnston