Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor.

@article{Guerlet2011SynthesisAB,
  title={Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor.},
  author={Guillaume Guerlet and T. Spangenberg and A. Mann and H. Faure and M. Ruat},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2011},
  volume={21 12},
  pages={
          3608-12
        }
}
Desmethylveramiline (1), an aza steroid analogue of veramiline was designed as a surrogate for cyclopamine, a reference antagonist of the Sonic Hedgehog (Shh) pathway. Desmethyveramiline (1) was prepared in seven steps from commercially available Fernholtz acid using the hydroformylation of a terminal olefine as the key step for the construction of the piperidine appendage. In two assays (i) the inhibition of the Shh-induced Gli-dependent luciferase activity in Shh-light2 cells, (ii) the… Expand
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