Linked parallel synthesis and MTT bioassay screening of substituted chalcones.

2.50
Hdl Handle:
http://hdl.handle.net/10541/85590
Title:
Linked parallel synthesis and MTT bioassay screening of substituted chalcones.
Authors:
Lawrence, Nicholas J; Rennison, David; McGown, Alan T; Ducki, Sylvie W; Gul, Lubna A; Hadfield, John A; Khan, Nader
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.
Affiliation:
Department of Chemistry, University of Manchester Institute of Science and Technology, P.O. Box 88, Manchester, M60 1QD, UK. Lawrencenj1@cardiff.ac.uk
Citation:
Linked parallel synthesis and MTT bioassay screening of substituted chalcones., 3 (5):421-6 J Comb Chem
Journal:
Journal of Combinatorial Chemistry
Issue Date:
2001
URI:
http://hdl.handle.net/10541/85590
DOI:
10.1021/cc000075z
PubMed ID:
11549359
Type:
Article
Language:
en
ISSN:
1520-4766
Appears in Collections:
All Paterson Institute for Cancer Research

Full metadata record

DC FieldValue Language
dc.contributor.authorLawrence, Nicholas Jen
dc.contributor.authorRennison, Daviden
dc.contributor.authorMcGown, Alan Ten
dc.contributor.authorDucki, Sylvie Wen
dc.contributor.authorGul, Lubna Aen
dc.contributor.authorHadfield, John Aen
dc.contributor.authorKhan, Naderen
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.en
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

Related articles on PubMed

All Items in Christie are protected by copyright, with all rights reserved, unless otherwise indicated.