SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL NOR-SECO ANALOGS OF TAXOL AND TAXOTERE

Novel nor-seco analogs of taxol and taxotere are synthesized from 14-h ydroxy-10-deacetylbaccatin III through periodic acid oxidation and NaB H3CN reduction, followed by coupling with the C-13 side chain precurso rs using a highly efficient beta-lactam synthon method. The new reduce d structure analogs show muted cytotoxicity against human cancer cell lines compared with taxol but still retain a certain level of activity despite the destruction of the A ring.