The interaction of chalcones with tubulin.
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 prepared and assessed for their ability to inhibit cell growth in vitro. The cytotoxicity correlates with their ability to bind to tubulin as measured by immunofluorescence, cell cycle analysis and disruption of microtubule assembly. Some of the chalcones were shown to bind to the type II oestrogen receptor.
Lawrence
N J
NJ
Department of Chemistry, University of Manchester Institute of Science and Technology, UK. n.lawrence@umist.ac.uk
McGown
A T
AT
Ducki
S
S
Hadfield
J A
JA
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002453:Cell Cycle / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000633:toxicity; D002522:Chlorocebus aethiops; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D020014:K562 Cells; D008870:Microtubules / Q000187:drug effects / Q000648:ultrastructure; D015394:Molecular Structure; D011427:Propiophenones / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D013552:Swine; D014404:Tubulin / Q000187:drug effects*; D014709:Vero Cells
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D011427:Propiophenones; D014404:Tubulin; D002599:Chalcone