Linked parallel synthesis and MTT bioassay screening of substituted chalcones.
Lawrence, Nicholas J Rennison, David McGown, Alan T Ducki, Sylvie W Gul, Lubna A Hadfield, John A Khan, Nader
Lawrence, Nicholas J
Rennison, David
McGown, Alan T
Ducki, Sylvie W
Gul, Lubna A
Hadfield, John A
Khan, Nader
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Abstract
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.
Description
Date
2001
Publisher
Collections
Keywords
Cultured Tumour Cells
Type
Article
Citation
Linked parallel synthesis and MTT bioassay screening of substituted chalcones., 3 (5):421-6 J Comb Chem