New Taxol (paclitaxel) prodrugs designed for ADEPT and PMT strategies in cancer chemotherapy |
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Authors: | Alaoui Abdessamad El Saha Nabendu Schmidt Frédéric Monneret Claude Florent Jean-Claude |
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Affiliation: | UMR 176 CNRS/Institut Curie, Centre de Recherche, 26 rue d'Ulm, 75248 Paris Cedex 05, France. |
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Abstract: | 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 beta-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. |
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