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

European Journal of Medicinal Chemistry
Florian HamonS Papot

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.

Citations

Sep 4, 2012·Archives of Pharmacal Research·Jeong In YunJongkook Lee
Jul 13, 2013·European Journal of Medicinal Chemistry·Thibaut LegiganSébastien Papot
Nov 8, 2014·Phytochemistry Reviews : Proceedings of the Phytochemical Society of Europe·Christopher M Chandler, Owen M McDougal
Oct 5, 2014·Journal of Molecular Neuroscience : MN·Souheyla BensalmaJean Marc Muller
Jan 10, 2018·Medicinal Research Reviews·Minhang XinBinghe Wang
Nov 2, 2011·Organic & Biomolecular Chemistry·Brigitte RenouxSébastien Papot
Jul 24, 2014·Molecular Cancer Therapeutics·Anaïs BalbousLucie Karayan-Tapon

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