Potent antimitotic and cell growth inhibitory properties of substituted chalcones.
A series of substituted chalcones was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. (E)-3-(3"-Hydroxy-4"-methoxyphenyl)-2-methyl-1-(3',4',5'- trimethoxyphenyl)-prop-2-en-1-one [IC50 (K562) 0.21 nM] was found to be the most active. A relationship between the conformation and cytotoxicity of the chalcones is discussed.
Ducki
S
S
Dept. of Chemistry, University of Manchester Institute of Science and Technology, UK.
Forrest
R
R
Hadfield
J A
JA
Kendall
A
A
Lawrence
N J
NJ
McGown
A T
AT
Rennison
D
D
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* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D018360:Crystallography, X-Ray; D015195:Drug Design; D006801:Humans; D020014:K562 Cells; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D002599:Chalcone