(Hydroxymethyl)acylfulvene: An Illudin Derivative with Superior Antitumor Properties

摘要: Reaction of the fungal sesquiterpene illudin S with excess paraformaldehyde in dilute H2SO4 gives (hydroxymethyl)acylfulvene. The primary allylic hydroxyl thus formed can undergo very facile replacement by a variety nucleophiles. (Hydroxymethyl)acylfulvene (MGI.114) was more toxic than precursor, acylfulvene, but less parent compound to HL 60 cells.