Total synthesis and absolute stereochemistry of the proteasome inhibitors cystargolides A and B.

  title={Total synthesis and absolute stereochemistry of the proteasome inhibitors cystargolides A and B.},
  author={Rodolfo Tello-Aburto and Liam P. Hallada and Doleshwar Niroula and Snezna Rogelj},
  journal={Organic \& biomolecular chemistry},
  volume={13 40},
The absolute stereochemistry of the cystargolides was determined by total synthesis. Evaluation of synthetic cystargolides and derivatives showed that the natural (2S,3R) stereochemistry is essential for activity. Moreover, benzyl esters (-)-10 and (-)-15 were found to be about 100 times more potent, and to selectively kill MCF-7 cancerous cells. 
7 Citations
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