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A new paclitaxel prodrug for use in ADEPT strategy
Emmanuel Bouvier1, Sylvie Thirot, Frédéric Schmidt
1UMR 176 CNRS-Institut Curie, Section Recherche 26 rue d'Ulm, 75248 Paris Cedex 05, France.
Organic & Biomolecular Chemistry
|October 31, 2003
Abstract:
A new paclitaxel prodrug intended for use in Antibody-Directed Prodrug Therapy (ADEPT) or Prodrug Monotherapy (PMT) has been prepared. This prodrug was originally designed to be activated into the drug by human beta-glucuronidase. In order to enhance the liberation rate of paclitaxel, an elongated spacer system including a nitro-aromatic derivative and a N,N'-methylethylenediamine was incorporated between the sugar moiety and the drug. Indeed, this new prodrug proved to be activated significantly faster than a former paclitaxel prodrug containing a conventional spacer.