Ducki S, Forrest R, Hadfield J A, Kendall A, Lawrence N J, McGown A T, Rennison D
Dept. of Chemistry, University of Manchester Institute of Science and Technology, UK.
Bioorg Med Chem Lett. 1998 May 5;8(9):1051-6. doi: 10.1016/s0960-894x(98)00162-0.
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.
合成了一系列取代查耳酮，并筛选了它们对K562人白血病细胞系的细胞毒性活性。发现（E）-3-（3″-羟基-4″-甲氧基苯基）-2-甲基-1-（3′,4′,5′-三甲氧基苯基）-丙-2-烯-1-酮[IC50（K562）0.21 nM]是活性最高的。讨论了查耳酮的构象与细胞毒性之间的关系。
