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Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors

  • Autori: Romagnoli, R.; Baraldi, P.; Sarkar, T.; Carrion, M.; Cara, C.; CRUZ LOPEZ, O.; Preti, D.; Tabrizi, M.; Tolomeo, M.; Grimaudo, S.; DI CRISTINA, A.; Zonta, N.; Balzarini, J.; Brancale, A.; Hsieh, H.; Hamel, E.
  • Anno di pubblicazione: 2008
  • Tipologia: Articolo in rivista
  • OA Link:


The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.