A new paclitaxel prodrug for use in ADEPT strategy.
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.
Bouvier
Emmanuel
E
UMR 176 CNRS-Institut Curie, Section Recherche 26 rue d'Ulm, 75248 Paris Cedex 05, France.
Thirot
Sylvie
S
Schmidt
Frédéric
F
Monneret
Claude
C
D000818:Animals; D045744:Cell Line, Tumor; D015195:Drug Design; D005966:Glucuronidase / Q000378:metabolism; D006801:Humans; D007167:Immunotherapy; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D017239:Paclitaxel / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*
D011355:Prodrugs; D005966:Glucuronidase; D017239:Paclitaxel