The chalcone 3,4,3',4',5'-pentamethoxychalcone is a potent cytotoxic agent.
A series of chalcones and (E)-4-(4'-hydroxyphenyl)but-3-en-2-one were prep
ared and assessed for their ability to inhibit cell growth in vitro. The cy
totoxicity correlates with their ability to bind to tubulin as measured by
immunofluorescence, cell cycle analysis and disruption of microtubule assem
bly. Some of the chalcones were shown to bind to the type II oestrogen rece
ptor.