A doxorubicin prodrug activated by the staudinger reaction.

Much effort has been devoted to prodrug systems that effect drug release at the tumor through enzymatic action. To widen the scope of prodrug therapy, the use of the selective Staudinger reaction as prodrug activator, instead of relying on enzymatic action, was investigated. Doxorubicin was conjugated to a p-azidobenzyl trigger that is cleaved after reacting with the chemical activator, triphenylphosphine.