Structure-activity studies on the lycorine pharmacophore: A potent inducer of apoptosis in human leukemia cells Academic Article uri icon

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abstract

  • The direct chemoselective differential functionalization of the ring-C hydroxyl groups present in the Amaryllidaceae alkaloid lycorine is described allowing for selective manipulation of the 1,2-hydroxyl groups. A mini-library comprised of synthetic and natural lycorane alkaloids was prepared and their apoptosis-inducing activity investigated in human leukemia (Jurkat) cells. Further insights into the nature of this interesting apoptosis-inducing pharmacophore are described, including the requirement of both free hydroxyl groups in ring-C.

authors

  • Mcnulty, James
  • Nair, Jerald J
  • Bastida, Jaume
  • Pandey, Siyaram
  • Griffin, Carly

publication date

  • May 2009