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dc.contributor.authorLawrence, Nicholas J
dc.contributor.authorRennison, David
dc.contributor.authorMcGown, Alan T
dc.contributor.authorDucki, Sylvie W
dc.contributor.authorGul, Lubna A
dc.contributor.authorHadfield, John A
dc.contributor.authorKhan, Nader
dc.date.accessioned2009-11-06T16:41:34Z
dc.date.available2009-11-06T16:41:34Z
dc.date.issued2001
dc.identifier.citationLinked parallel synthesis and MTT bioassay screening of substituted chalcones., 3 (5):421-6 J Comb Chemen
dc.identifier.issn1520-4766
dc.identifier.pmid11549359
dc.identifier.doi10.1021/cc000075z
dc.identifier.urihttp://hdl.handle.net/10541/85590
dc.description.abstractA 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.
dc.language.isoenen
dc.subjectCultured Tumour Cellsen
dc.subject.meshAcetophenones
dc.subject.meshAntineoplastic Agents
dc.subject.meshChalcone
dc.subject.meshCombinatorial Chemistry Techniques
dc.subject.meshDrug Screening Assays, Antitumor
dc.subject.meshHumans
dc.subject.meshMagnetic Resonance Spectroscopy
dc.subject.meshReproducibility of Results
dc.subject.meshTetrazolium Salts
dc.subject.meshThiazoles
dc.subject.meshTumor Cells, Cultured
dc.titleLinked parallel synthesis and MTT bioassay screening of substituted chalcones.en
dc.typeArticleen
dc.contributor.departmentDepartment of Chemistry, University of Manchester Institute of Science and Technology, P.O. Box 88, Manchester, M60 1QD, UK. Lawrencenj1@cardiff.ac.uken
dc.identifier.journalJournal of Combinatorial Chemistryen
html.description.abstractA 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.


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