Synthesis of 7- and 10-spermine conjugates of paclitaxel and 10-deacetyl-paclitaxel as potential prodrugs

摘要

Efficient syntheses of two taxol analogs bearing the linear polyamine spermine at 7- and 10-positions of paclitaxel and 10-deacetyl-paclitaxel have been developed.These polyamine-taxol-conjugates were isolated as water soluble difluoride salts.The aim of the present work was to introduce a chemical modification into taxol skeleton in order to increase drug selectivity toward tumor cells.The cytotoxic activity of these conjugates was evaluated in MCF7 and MCF7-R cell lines.The observed low cytotoxicity suggests that these conjugates could act as potential prodrugs.