(HYDROXYMETHYL)ACYLFULVENE - AN ILLUDIN DERIVATIVE WITH SUPERIOR ANTITUMOR PROPERTIES

Reaction of the fungal sesquiterpene illudin S with excess paraformald ehyde in dilute H2SO4 gives (hydroxymethyl)acylfulvene. The primary al lylic hydroxyl thus formed can undergo very facile replacement by a va riety of nucleophiles. (Hydroxymethyl)acylfulvene (MGI.114) was more t oxic than a precursor, acylfulvene, but less toxic than the parent com pound illudin S to HL 60 cells.