Linked parallel synthesis and MTT bioassay screening of substituted chalcones.
AuthorsLawrence, Nicholas J
McGown, Alan T
Ducki, Sylvie W
Gul, Lubna A
Hadfield, John A
AffiliationDepartment of Chemistry, University of Manchester Institute of Science and Technology, P.O. Box 88, Manchester, M60 1QD, UK. Lawrencenj1@cardiff.ac.uk
MetadataShow full item record
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.
CitationLinked parallel synthesis and MTT bioassay screening of substituted chalcones., 3 (5):421-6 J Comb Chem
JournalJournal of Combinatorial Chemistry
- Synthesis and anti-proliferative activity of fluoro-substituted chalcones.
- Authors: Burmaoglu S, Algul O, Anıl DA, Gobek A, Duran GG, Ersan RH, Duran N
- Issue date: 2016 Jul 1
- Synthetic and biological activity evaluation studies on novel 1,3-diarylpropenones.
- Authors: Mukherjee S, Kumar V, Prasad AK, Raj HG, Bracke ME, Olsen CE, Jain SC, Parmar VS
- Issue date: 2001 Feb
- Antitumor agents. Part 202: novel 2'-amino chalcones: design, synthesis and biological evaluation.
- Authors: Xia Y, Yang ZY, Xia P, Bastow KF, Nakanishi Y, Lee KH
- Issue date: 2000 Apr 17
- Efficient liquid-phase synthesis of 2'-hydroxychalcones.
- Authors: Stoyanov EV, Champavier Y, Simon A, Basly JP
- Issue date: 2002 Oct 7
- Synthesis of isomeric, oxathiolone fused chalcones, and comparison of their activity toward various microorganisms and human cancer cells line.
- Authors: Konieczny MT, Konieczny W, Sabisz M, Skladanowski A, Wakieć R, Augustynowicz-Kopeć E, Zwolska Z
- Issue date: 2007 May