| Literature DB >> 16554162 |
Abdessamad El Alaoui1, Nabendu Saha, Frédéric Schmidt, Claude Monneret, Jean-Claude Florent.
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.Entities:
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Year: 2006 PMID： 16554162 DOI： 10.1016/j.bmc.2006.03.002
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641