Synthesis and biological evaluation of novel 9-functional heterocyclic coupled 7-deoxy-9-Dihydropaclitaxel analogue

Novel 9-functional heterocyclic coupled 7-deoxy-9-dihydropaclitaxel analogues Scheme 1 and Scheme 2 synthesized from a natural taxoid 5-cinnamoyltriacetyltaxicin-I ( Chart 1 and Scheme 1) and their biological evaluation in tubulin assembly activity and cytotoxicity in vitro against several human tumor cell lines are first presented. The biologically tested results show that Scheme 1 and Scheme 2 are inactive in tubulin assembly assay and have no more remarkable cytotoxicities against human tumor cell lines SK-0V3, WIDR and MCF-7, though 22 and 23 exhibit more potent cytotoxicity against human liver cancer and human esophagus cancer cell lines (BEL-7402 and ECa-109) than paclitaxel.