Title: Synthesis and Evaluation of p-Nitrophenylβ-D-Glucopyranosiduronic Analogues as New Triggers for β-Glucuronidase Mediated Prodrug Mono- Therapy
VOLUME: 2 ISSUE: 8
Author(s):Damien Combaud, Mickael Thomas, Sebastien Papot and Jean-Pierre Gesson
Affiliation:UMR 6514: Synthese et Reactivite des Substances Naturelles, Universite de Poitiers et CNRS, 40,Av. du Recteur Pineau, F-86022 Poitiers, France.
Keywords:Cancer, chemotherapy, prodrug, A.D.E.P.T., P.M.T., β-glucuronidase, trigger, β-D-glucuronide
Abstract: Four new p-nitrophenyl β-D-glucuronide analogues, potentially useful as new triggers for β- glucuronidase mediated P.M.T. (Prodrug Mono-Therapy), have been prepared in a few steps. These compounds were tested for hydrolysis in the presence of either Escherichia Coli or bovine liver β-glucuronidase. The KM and Vmax values obtained for each analogue are reported.
