Potent antimitotic and cell growth inhibitory properties of substituted chalcones

被引:359
作者
Ducki, S
Forrest, R
Hadfield, JA
Kendall, A
Lawrence, NJ
McGown, AT
Rennison, D
机构
[1] Univ Manchester, Inst Sci & Technol, Dept Chem, Manchester M60 1QD, Lancs, England
[2] Christie Hosp NHS Trust, Paterson Inst Canc Res, CRC, Dept Drug Dev, Manchester M20 4BX, Lancs, England
关键词
antitumour compounds; chalcones; molecular modelling/mechanics; X-ray crystal structures;
D O I
10.1016/S0960-894X(98)00162-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1051 / 1056
页数:6
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