1198184-89-2Relevant academic research and scientific papers
Cyclopamine analogs bearing exocyclic methylenes are highly potent and acid-stable inhibitors of hedgehog signaling
Moschner, Johann,Chentsova, Anna,Eilert, Nicole,Rovardi, Irene,Heretsch, Philipp,Giannis, Athanassios
, p. 2328 - 2335 (2013)
The chemical synthesis and biological evaluation of new cyclopamine analogs bearing exocyclic methylenes in different positions is described. Bis-exo-cyclopamine 6 was identified as a potent inhibitor of the Gli1-dependent luciferase expression in Shh-LIGHTII cells. An extension of this study to F-ring-modified structures shows the necessity of a rigidly positioned nitrogen atom for bioactivity as well as the presence of the C21 methyl group for acid stability and bioactivity.
Synthesis of cyclopamine using a biomimetic and diastereoselective approach
Giannis, Athanassios,Heretsch, Philipp,Sarli, Vasiliki,Stoessel, Anne
supporting information; experimental part, p. 7911 - 7914 (2010/03/30)
From Homer to hedgehog: Cyclopamine, the first inhibitor of the hedgehog signaling pathway, causes cyclopia in embryos butin adults it is a potent anticancer drug. A concise biomimetic and diastereoselective synthesis of cyclopamine (2) starting from comm
