Title: Design, synthesis, and biological evaluation of thiophene analogues of chalcones
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Carrion, Maria Dora
Cara, Carlota Lopez
Cruz-Lopez, Olga
Preti, Delia
Tolomeo, Manlio
Grimaudo, Stefania
Di Cristina, Antonella
Zonta, Nicola
Balzarini, Jan
Brancale, Andrea
Sarkar, Taradas
Hamel, Ernest #
Issue Date: May-2008
Publisher: Pergamon-elsevier science ltd
Series Title: Bioorganic & medicinal chemistry vol:16 issue:10 pages:5367-5376
Abstract: Chalcones are characterized by possessing an enone moiety between two aromatic rings. A series of chalcone-like agents, in which the double bond of the enone system is embedded within a thiophene ring, were synthesized and evaluated for antiproliferative activity and inhibition of tubulin assembly and colchicine binding to tubulin. The replacement of the double bond with a thiophene maintains antiproliferative activity and therefore must not significantly alter the relative conformation of the two aryl rings. The synthesized compounds were found to inhibit the growth of several cancer cell lines at nanomolar to low micromolar concentrations. In general, all compounds having significant antiproliferative activity inhibited tubulin polymerization with an IC50 < 2 mu M. Several of these compounds caused K562 cells to arrest in the G2/M phase of the cell cycle. (C) 2008 Elsevier Ltd. All rights reserved.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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