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Linked parallel synthesis and MTT bioassay screening of substituted chalcones

Lawrence, NJ, Rennison, D, McGown, AT, Ducki, S, Gul, LA, Hadfield, JA and Khan, N 2001, 'Linked parallel synthesis and MTT bioassay screening of substituted chalcones' , Journal of Combinatorial Chemistry, 3 (5) , pp. 421-426.

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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 IC50 less than 1 M 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.

Item Type: Article
Themes: Subjects / Themes > Q Science > Q Science (General)
Subjects / Themes > Q Science > QD Chemistry
Subjects outside of the University Themes
Schools: Colleges and Schools > College of Science & Technology
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences > Biomedical Research Centre
Journal or Publication Title: Journal of Combinatorial Chemistry
Publisher: American Chemical Society
Refereed: Yes
ISSN: 15204766
Depositing User: H Kenna
Date Deposited: 07 Aug 2007 14:47
Last Modified: 20 Aug 2013 16:45
URI: http://usir.salford.ac.uk/id/eprint/148

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