Recent advances in the chemistry of taxol

The history of the development of the important anticancer drug taxol (1) i s briefly described, and recent studies of its chemistry and tubulin-bindin g conformation are then presented. Topics discussed include side chain atta chment to baccatin III (3a), the effect of oxygenation of the taxane ring s ystem on bioactivity, the importance of the oxetane ring for bioactivity, t he synthesis of a C-6/C-4 bridged analogue, and the conformation of the sid e chain when taxol is bound in a complex with polymerized tubulin.