Synthesis and Structure-Activity Relationships of Novel Nor-Seco Analogs of Taxol and Taxotere

Abstract

Novel nor-seco analogs of taxol and taxotere are synthesized from 14-hydroxy-10-deacetylbaccatin III through periodic acid oxidation and NaBH 3 CN reduction, followed by coupling with the C-13 side chain precursors using a highly efficient β-lactam synthon method. The new reduced structure analogs show muted cytotoxicity aganist human cancer cell lines compared with taxol but still retain a certain level of activity despite the destruction of the A ring