Wortmannin-C20 conjugates generate wortmannin.

@article{Yuan2006WortmanninC20CG,
  title={Wortmannin-C20 conjugates generate wortmannin.},
  author={Hushan Yuan and Ji Luo and Ralph Weissleder and Lewis C. Cantley and Lee Josephson},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 2},
  pages={740-7}
}
We report on C20-6-(N-methylamino)hexanoic conjugates of wortmannin featuring a tertiary enamine attached to the C20 that inhibit phosphoinositol-3-OH kinase (PI3K) by producing wortmannin (Wm) through an intramolecular attack. The generation of Wm by these conjugates permits the design of Wm based PI3K inhibitors that need not fit into the ATP pocket of PI3K, including Wm conjugates of BSA, IgG, or beads. Wm generating WmC20-N(Me)-hexanoate conjugates offer an approach to the design of… CONTINUE READING

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