New Taxol® (paclitaxel) prodrugs designed for ADEPT and PMT strategies in cancer chemotherapy Original Research Article

Two new glucuronide paclitaxel prodrugs have been synthesized. Linked to the 2′-OH of the drug by a carbonate function, they include a self-immolative spacer bearing an arylnitro or arylamino group between the drug and the glucuronic acid residue. Both prodrugs were well detoxified and easily cleaved in the presence of β-d-glucuronidase with fast removal of the spacer, releasing paclitaxel. The arylamino spacer-containing prodrug, more stable than the corresponding nitro analogue, was selected for further studies.