Title: Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Carrion, Maria Dora
Lopez Cara, Carlota
Preti, Delia
Fruttarolo, Francesca
Pavani, Maria Giovanna
Tabrizi, Mojgan Aghazadeh
Tolomeo, Manlio
Grimaudo, Stefania
Di Cristina, Antonella
Balzarini, Jan
Hadfield, John A
Brancale, Andrea
Hamel, Ernest #
Issue Date: May-2007
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:50 issue:9 pages:2273-2277
Abstract: Two new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene molecular skeleton and its 3-amino positional isomer were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. Although many more 3-amino derivatives have been synthesized so far, the most promising compound in this series was 2-amino-6-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]thiophene, which inhibits cancer cell growth at subnanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.
ISSN: 0022-2623
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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