1366596-67-9Relevant academic research and scientific papers
A new cyclopamine glucuronide prodrug with improved kinetics of drug release
Renoux, Brigitte,Legigan, Thibaut,Bensalma, Souheyla,Chadeneau, Corinne,Muller, Jean-Marc,Papot, Sebastien
, p. 8459 - 8465 (2011)
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. The Royal Society of Chemistry 2011.
