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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Evaluation of p-Nitrophenylβ-D-Glucopyranosiduronic Analogues as New Triggers for β-Glucuronidase Mediated Prodrug Mono- Therapy

Author(s): Damien Combaud, Mickael Thomas, Sebastien Papot and Jean-Pierre Gesson

Volume 2, Issue 8, 2005

Page: [631 - 637] Pages: 7

DOI: 10.2174/157018005774717271

Price: $65


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.

Keywords: Cancer, chemotherapy, prodrug, A.D.E.P.T., P.M.T., β-glucuronidase, trigger, β-D-glucuronide

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