Search

Research was conducted to examine the biological activity and semisynthesis of paclitaxel (Taxol) analogues, namely, 5,20-thiapaclitaxel analogue and the 5,20-selenapaclitaxel analogue, whose oxygen atom in ring D is substituted by a selenium or a sulfur atom. Results suggest that the substitution of a sulfur for the oxygen of the oxetane ring in paclitaxel leads to a significant diminution of its tubulin-assembly activity and cytotoxicity. Findings also demonstrate that the activity loss is not caused by any basicity of the heteroatom.

Discusses the conversion of cephalomannine to paclitaxel and 3'N-acyl-3'-N-debenzoylpaclitaxel analogs. Paclitaxel acquired from T. brevifolia bark; Similar chromatographic properties of paclitaxel and cephalomannine.