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