取代查尔酮的连接平行合成及MTT生物活性检测筛选
Linked parallel synthesis and MTT bioassay screening of substituted chalcones.
作者信息
Lawrence N J, Rennison D, McGown A T, Ducki S, Gul L A, Hadfield J A, Khan N
机构信息
Department of Chemistry, University of Manchester Institute of Science and Technology, P.O. Box 88, Manchester, M60 1QD, UK.
出版信息
J Comb Chem. 2001 Sep-Oct;3(5):421-6. doi: 10.1021/cc000075z.
A 644-membered library of chalcones was prepared by parallel synthesis using the Claisen-Schmidt base-catalyzed aldol condensation of substituted acetophenones and benzaldehydes. The cytotoxicity of these chalcones was conveniently determined upon the crude products directly in 96-well microtiter test plates by the conventional MTT assay. This method revealed seven chalcones of IC(50) less than 1 microM of which 4'-hydroxy-2,4,6,3'-tetramethoxychalcone (5a) was the most active [IC(50) (K562), 30 nM]; it causes cell cycle arrest at the G(2)/M point and binds to tubulin at the colchicine binding site.
通过克莱森-施密特碱催化取代苯乙酮与苯甲醛的羟醛缩合反应，采用平行合成法制备了一个由644个查尔酮组成的文库。这些查尔酮的细胞毒性可通过传统的MTT法在96孔微量滴定板中直接对粗产物进行方便地测定。该方法揭示了7种IC(50)小于1微摩尔的查尔酮，其中4'-羟基-2,4,6,3'-四甲氧基查尔酮（5a）活性最高[IC(50)（K562），30纳摩尔]；它导致细胞周期在G(2)/M期停滞，并在秋水仙碱结合位点与微管蛋白结合。
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