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Issue 24, 2011
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A new cyclopamine glucuronide prodrug with improved kinetics of drug release

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Abstract

We prepared a new glucuronide prodrug of cyclopamine designed to target selectively the Hedgehog signalling pathway of cancer cells. This prodrug includes a novel self-immolative linker bearing a hydrophilic side chain that can be easily introduced via “click chemistry”. With this design, the prodrug exhibits reduced toxicity compared to the free drug on U87 glioblastoma cells. However, in the presence of β-glucuronidase, the prodrug conducts to the quick release of cyclopamine thereby restoring its antiproliferative activity.

Graphical abstract: A new cyclopamine glucuronide prodrug with improved kinetics of drug release

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Publication details

The article was received on 04 Jul 2011, accepted on 19 Sep 2011 and first published on 19 Sep 2011


Article type: Paper
DOI: 10.1039/C1OB06081C
Citation: Org. Biomol. Chem., 2011,9, 8459-8464
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    A new cyclopamine glucuronide prodrug with improved kinetics of drug release

    B. Renoux, T. Legigan, S. Bensalma, C. Chadéneau, J. Muller and S. Papot, Org. Biomol. Chem., 2011, 9, 8459
    DOI: 10.1039/C1OB06081C

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