Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma. - Archive ouverte HAL
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2010

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

Résumé

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.

Dates et versions

hal-00582528 , version 1 (01-04-2011)

Identifiants

Citer

Florian Hamon, Brigitte Renoux, Corinne Chadéneau, Jean-Marc Muller, Sébastien Papot. Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma.. European Journal of Medicinal Chemistry, 2010, 45 (4), pp.1678-82. ⟨10.1016/j.ejmech.2009.12.067⟩. ⟨hal-00582528⟩
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