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.

Design, synthesis, and antitumor evaluation of a series of bile acid–polyamine–AZT phosphoramidate conjugates are reported.Figure optionsDownload as PowerPoint slide