Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins.

@article{Desrat2015DevelopmentOA,
  title={Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins.},
  author={S. Desrat and C. Remeur and F. Roussi},
  journal={Organic & biomolecular chemistry},
  year={2015},
  volume={13 19},
  pages={
          5520-31
        }
}
The synthesis, on a large scale, with very good yield and er via an efficient strategy, of a chiral 4-substituted 2-cyclohexenone intermediate, was a milestone in the synthesis of seven analogues of meiogynin A, a natural sesquiterpenoid dimer. These compounds were elaborated in ten linear steps. Their binding affinities for Bcl-xL and Mcl-1, two proteins of the Bcl-2 family, overexpressed in various types of cancers, were evaluated. This enabled to further SAR studies en route to the… Expand
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