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Linked Parallel Synthesis and MTT Bioassay Screening of Substituted Chalcones

2001; American Chemical Society; Volume: 3; Issue: 5 Linguagem: Inglês

10.1021/cc000075z

1520-4774

Nicholas J. Lawrence, David Rennison, Alan T. McGown, Sylvie Ducki, Lubna A. Gul, John A. Hadfield, Nader Khan,

Synthesis and biological activity

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 IC50 less than 1 μM of which 4'-hydroxy-2,4,6,3'-tetramethoxychalcone (5a) was the most active [IC50 (K562), 30 nM]; it causes cell cycle arrest at the G2/M point and binds to tubulin at the colchicine binding site.