Linked parallel synthesis and MTT bioassay screening of substituted chalcones

Lawrence, NJ; Rennison, D; McGown, AT; Ducki, S; Gul, LA; Hadfield, JA; Khan, N

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.

Citation

Lawrence, N., Rennison, D., McGown, A., Ducki, S., Gul, L., Hadfield, J., & Khan, N. (2001). Linked parallel synthesis and MTT bioassay screening of substituted chalcones. Journal of Combinatorial Chemistry, 3(5), 421-426. https://doi.org/10.1021/cc000075z

• Journal Article Type: Article
• Publication Date: Sep 1, 2001
• Deposit Date: Aug 7, 2007
• Journal: Journal of Combinatorial Chemistry
• Print ISSN: 1520-4766
• Publisher: American Chemical Society
• Peer Reviewed: Peer Reviewed
• Volume: 3
• Issue: 5
• Pages: 421-426
• DOI: https://doi.org/10.1021/cc000075z
• Publisher URL: http://dx.doi.org/10.1021/cc000075z