Semisynthesis and screening of a small library of pro-apoptotic squamocin analogues: selection and study of a benzoquinone hybrid with an improved biological profile.

@article{Derbr2006SemisynthesisAS,
  title={Semisynthesis and screening of a small library of pro-apoptotic squamocin analogues: selection and study of a benzoquinone hybrid with an improved biological profile.},
  author={S{\'e}verine Derbr{\'e} and Romain Duval and Ga{\"e}l Rou{\'e} and Aurelio Garofano and Erwan Poupon and Ulrich Brandt and Santos A Susin and Reynald Hocquemiller},
  journal={ChemMedChem},
  year={2006},
  volume={1 1},
  pages={118-29}
}
Acetogenins of Annonaceae, including squamocin (1), exert spectacular cytotoxicity and the most potent inhibition of NADH:ubiquinone oxidoreductase known so far. Cell death induced by these natural products was identified as apoptosis and was thought to be linked to alterations in mitochondrial function. Quinone-squamocin hybrid compounds were semisynthesized and evaluated for their pro-apoptotic properties with a screening method based on dissipation of the mitochondrial transmembrane… CONTINUE READING