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.
Keywords: Cancer, chemotherapy, prodrug, A.D.E.P.T., P.M.T., β-glucuronidase, trigger, β-D-glucuronide
Letters in Drug Design & Discovery
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:
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.
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Cite this article as:
Combaud Damien, Thomas Mickael, Papot Sebastien and Gesson Jean-Pierre, Synthesis and Evaluation of p-Nitrophenylβ-D-Glucopyranosiduronic Analogues as New Triggers for β-Glucuronidase Mediated Prodrug Mono- Therapy, Letters in Drug Design & Discovery 2005; 2 (8) . https://dx.doi.org/10.2174/157018005774717271
DOI https://dx.doi.org/10.2174/157018005774717271 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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