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Keywords:

  • antimalarial agents;
  • medicinal chemistry;
  • natural products;
  • terpenoids;
  • total synthesis
Thumbnail image of graphical abstract

All sewn up: A “three-staged stitch” was used to append the A–C rings of desoxohexacyclinol (1), which was further converted into the related compounds hexacyclinol (2) and 5-epi-hexacyclinol (3). Screening of the late-staged intermediates indicated that precursors to 1 retain potent antimalarial activity. The mechanism of this action is suggested to involve a three-step prodrug-like activation.