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Synthesis and Biological Evaluation of 2- and 3-Aminobenzo[b]thiophene Derivatives as Antimitotic Agents and Inhibitors of Tubulin Polymerization.

  • Autori: Romagnoli, R.; Baraldi, P.; Carrion, M.; Cara, C.; Preti, D.; Fruttarolo, F.; Pavani, M.; Tabrizi, M.; Tolomeo, M.; Grimaudo, S.; DI CRISTINA, A.; Balzarini, J.; Hadfield, J.; Brancale, A.; Hamel, E.
  • Anno di pubblicazione: 2007
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • OA Link:


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.