Title: Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Sarkar, Taradas
Carrion, Maria Dora
Cruz-Lopez, Olga
Lopez Cara, Carlota
Tolomeo, Manlio
Grimaudo, Stefania
Di Cristina, Antonietta
Pipitone, Maria Rosaria
Balzarini, Jan
Gambari, Roberto
Ilaria, Lampronti
Saletti, Roberto
Brancale, Andrea
Hamel, Ernest #
Issue Date: Sep-2008
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:16 issue:18 pages:8419-8426
Abstract: Molecules that target microtubules have an important role in the treatment of cancer. A new class of inhibitors of tubulin polymerization based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. The most promising compound in this series was 2-(3,4,5-trimethoxybenzoyl)-3-dimethylamino-6-methoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.
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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