Six first-generation illudin analogs were tested for antitumor activit
y using in vitro cytotoxicity and in vivo xenograft models. One analog
, dehydroilludin M, inhibited xenograft growth and prolonged life span
of tumor bearing animals, when administered IP or IV whereas the pare
nt Illudin S compound was ineffective The efficacy of dehydroilludin M
in the MV522 lung carcinoma model exceeded that of 9 known anticancer
drugs, and equaled that of mitomycin C. Dehydroilludin M retained the
in vitro relative selective cytotoxicity for carcinomas and myeloid l
eukemia cell lines noted with the parent illudin compounds. In vitro c
ytotoxicity data predicted, response of xenografts. Dehydroilludin M a
lso retained the in vitro activity of the parent compounds against dif
ferent multidrug resistant mdr cell lines.