The Taxane Sinenxan A Chemical And Structural Modification

SIA is a new biosynthetic taxane. In order to search for new taxol analogues with cytotoxicity, SIA was studied and modified.A new taxoid with D—ring has been carried out by a reaction sequence of six steps. A more facile synthetic procedure has been put forward by studying and analyzing the features of the reactions involved.A number of new taxoids containing the tetrahydrofuran ring with a exocyclic double bound were esterified at C₁₄ or C₁₀ positions with taxol/taxotere side chain, preliminary pharmacological tests showed that all the compounds have cytotoxicity on KB, HCF8 cmd A2780. Meanwhile, the relationship between their structures and activity was discussed. The side chains of taxol and taxotere were synthesized stere-oselectively. Eighty—six compounds were synthesizd, sixty—one of which are new taxoids.