1012369-78-6Relevant articles and documents
Synthesis and biological evaluation of 1-methyl-2-(3′,4′, 5′-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors
Romagnoli, Romeo,Baraldi, Pier Giovanni,Sarkar, Taradas,Carrion, Maria Dora,Cara, Carlota Lopez,Cruz-Lopez, Olga,Preti, Delia,Tabrizi, Mojgan Aghazadeh,Tolomeo, Manlio,Grimaudo, Stefania,Di Cristina, Antonella,Zonta, Nicola,Balzarini, Jan,Brancale, Andrea,Hsieh, Hsing-Pang,Hamel, Ernest
, p. 1464 - 1468 (2008/09/20)
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.