Issue 1, 2012
From the journal:

MedChemComm

A self-immolative dendritic glucuronide prodrug of doxorubicin†

Marion Grinda,a   Jonathan Clarhaut,bc   Brigitte Renoux,a   Isabelle Tranoy-Opalinskia  and  Sébastien Papot*a  

* Corresponding authors

a Université de Poitiers, UMR-CNRS 6514, 4 rue Michel Brunet, BP 633, Poitiers, France
E-mail: sebastien.papot@univ-poitiers.fr
Fax: +33 549 453 501
Tel: +33 549 453 862

b Université de Poitiers, UMR-CNRS 6187, 1 rue Georges Bonnet, BP 633, Poitiers, France

c INSERM CIC 0802, 2 rue de la Milétrie, CHU de Poitiers, Poitiers, France

Abstract

The first self-immolative dendritic glucuronide prodrug of doxorubicin was studied with the aim to target β-glucuronidase overexpressed in the microenvironment of numerous tumors. This compound includes a chemical amplifier programmed to release two molecules of doxorubicin after a single enzymatic activation step. Upon β-glucuronidase activation, the dendritic prodrug was twice more toxic than its monomeric counterpart against H661 lung cancer cells.

Graphical abstract: A self-immolative dendritic glucuronide prodrug of doxorubicin

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Article information

DOI
https://doi.org/10.1039/C1MD00193K
Article type
Concise Article
Submitted
29 Jul 2011
Accepted
21 Sep 2011
First published
19 Oct 2011

Med. Chem. Commun., 2012,3, 68-70

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A self-immolative dendritic glucuronide prodrug of doxorubicin

M. Grinda, J. Clarhaut, B. Renoux, I. Tranoy-Opalinski and S. Papot, Med. Chem. Commun., 2012, 3, 68 DOI: 10.1039/C1MD00193K

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