Linked parallel synthesis and MTT bioassay screening of substituted chalcones

Lawrence, NJ, Rennison, D, McGown, AT, Ducki, S, Gul, LA, Hadfield, JA ORCID: https://orcid.org/0000-0001-7984-8319 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:	Schools > School of Environment and Life Sciences Schools > School of Environment and Life Sciences > Biomedical Research Centre
Journal or Publication Title:	Journal of Combinatorial Chemistry
Publisher:	ACS Publications
Refereed:	Yes
ISSN:	15204766
Depositing User:	H Kenna
Date Deposited:	07 Aug 2007 13:47
Last Modified:	27 Aug 2021 21:58
URI:	https://usir.salford.ac.uk/id/eprint/148

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