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Title: Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Carrion, Maria Dora
Cruz-Lopez, Olga
Cara, Carlota Lopez
Tolomeo, Manlio
Grimaudo, Stefania
Cristina, Antonietta Di
Pipitone, Maria Rosa
Balzarini, Jan
Kandil, Sahar
Brancale, Andrea
Sarkar, Taradas
Hamel, Ernest #
Issue Date: Sep-2008
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:18 issue:18 pages:5041-5045
Abstract: Microtubules are among the most successful targets of compounds potentially useful for cancer therapy. A new series of inhibitors of tubulin polymerization based on the 2-amino-3-(3,4,5-trimethoxybenzoyl)-4,5,6,7-tetrahydrothieno[b]pyridine 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-amino-3-(3,4,5-trimethoxybenzoyl)-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[b]pyridine, which inhibits cancer cell growth with IC(50)-values ranging from 25 to 90nM against a panel of four cancer cell lines, and interacts strongly with tubulin by binding to the colchicine site. In this series of N(6)-carbamate derivatives, any further increase in the length and in the size of the alkyl chain resulted in reduced activity.
URI: 
ISSN: 0960-894X
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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