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

Novel 9-functional heterocyclic coupled 7-deoxy-9-dihydropaclitaxel analogu es 17 and 22-24 synthesized from a natural taxoid 5-cinnamoyltriacetyltaxic in-I (3) and their biological evaluation in tubulin assembly activity and c ytotoxicity in vitro against several human tumor cell lines are first prese nted. The biologically tested results show that 17, 22 and 23 are inactive in tubulin assembly assay and have no more remarkable cytotoxicities agains t human tumor cell lines SK-0V3, WIDR and MCF-7, though 22 and 23 exhibit m ore potent cytotoxicity against human liver cancer and human esophagus canc er cell lines (BEL-7402 and ECa-109) than paclitaxel. (C) 2000 Elsevier Sci ence Ltd. All rights reserved.