The crude organic extract of Dendropanax arboreus was selected as a ca
ndidate for bioassay-guided fractionation on the basis of its relative
ly selective cytotoxicity to a subset of cell lines within the Nationa
l Cancer Institute's disease-oriented in vitro tumor-screening panel.
The major compound responsible for the in vitro cytotoxicity was falca
rinol (1). Several other known compounds were isolated and found to be
cytotoxic, including dehydrofalcarinol (2), a diynene (3), falcarindi
ol (4), and dehydrofalcarindiol (5). In addition, two novel polyacetyl
enes, dendroarboreols A (6) and B (7), were isolated and characterized
by standard and inverse-detected NMR methods. Compounds were selected
from this series for absolute stereochemical determination using the
modified Mosher method and preliminary in vivo evaluation using a LOX
melanoma mouse xenograft model.