Design, synthesis, and antitumor activity of bile acid–polyamine–nucleoside conjugates

A series of bile acid–polyamine amides conjugated with 3′-azido-3′-deoxythymidine (AZT) as potential antitumor prodrugs in the form of phosphoramidates were synthesized in good yields and their antitumor activities were assayed against two human cancer cells in vitro: cervix cancer HeLa cells and renal cancer 7860 cells. The improved antitumor activity probably derived from the enhanced delivery efficiency of AZT due to bile acid–polyamine conjugates.