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Keywords:

  • inhibitors;
  • LY294002;
  • phosphatidylinositol 3-kinase;
  • PI3K;
  • prodrugs;
  • tetrazoles
Thumbnail image of graphical abstract

Prodrugs for PI3K: A series of substituted analogues of the phosphatidylinositol 3 kinase (PI3K) inhibitor LY294002 were prepared and found to potently inhibit the isolated enzyme but not MCF7 cell proliferation. Two tetrazolyl-substituted analogues were further derivatized as prodrugs resulting in restoration of cell-based activity. These data provide a conceptual model for development of tumor-targeting prodrug forms of cell-impermeable PI3K inhibitors.