Synthesis of novel beta-lactone inhibitors of fatty acid synthase.

  title={Synthesis of novel beta-lactone inhibitors of fatty acid synthase.},
  author={Robyn D. Richardson and Gil Ma and Yatsandra Oyola and Manuel A Zancanella and Lynn M. Knowles and Piotr Cieplak and Daniel Romo and Jeffrey W. Smith},
  journal={Journal of medicinal chemistry},
  volume={51 17},
Fatty acid synthase (FAS) is necessary for growth and survival of tumor cells and is a promising drug target for oncology. Here, we report on the syntheses and activity of novel inhibitors of the thioesterase domain of FAS. Using the structure of orlistat as a starting point, which contains a beta-lactone as the central pharmacophore, 28 novel congeners were synthesized and examined. Structural features such as the length of the alpha- and beta-alkyl chains, their chemical composition, and… CONTINUE READING
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