TY - JOUR
T1 - Synthesis and Biological Evaluation of 2- and 3-Aminobenzo[b]thiophene Derivatives as Antimitotic Agents and Inhibitors of Tubulin Polymerization.
AU - Grimaudo, Stefania
AU - Cara, Carlota Lopez
AU - Hamel, Ernest
AU - Tabrizi, Mojgan Aghazadeh
AU - Balzarini, Jan
AU - Fruttarolo, Francesca
AU - Brancale, Andrea
AU - Preti, Delia
AU - Pavani, Maria Giovanna
AU - Carrion, Maria Dora
AU - Hadfield, John A.
AU - Baraldi, Pier Giovanni
AU - Romagnoli, Romeo
AU - Di Cristina, Antonietta
PY - 2007
Y1 - 2007
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10447/27728
M3 - Article
SN - 0022-2623
VL - 50
SP - 2273
EP - 2277
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
ER -