2. Academic Validation
  3. Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma

Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma

  • Eur J Med Chem. 2010 Apr;45(4):1678-82. doi: 10.1016/j.ejmech.2009.12.067.
Florian Hamon 1,  Brigitte Renoux,  Corinne Chadéneau,  Jean-Marc Muller,  Sébastien Papot
Affiliations

Affiliation

  • 1 Université de Poitiers, UMR-CNRS 6514, 40 avenue du Recteur Pineau, 86022 Poitiers, France.
PMID: 20116904 DOI: 10.1016/j.ejmech.2009.12.067
Abstract

The first glucuronide prodrug of the Hedgehog signaling inhibitor cyclopamine was synthesized. The carbamoyl derivatisation of cyclopamine significantly decreased its toxicity towards the U87 human glioblastoma cell line. However, when the prodrug was incubated with beta-glucuronidase in the culture media, the active drug was efficiently released thereby restoring its anti-proliferative activity.

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