TY - JOUR
T1 - Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors
AU - Grimaudo, Stefania
AU - Cara, Carlota Lopez
AU - Cruz-Lopez, Olga
AU - Zonta, Nicola
AU - Sarkar, Taradas
AU - Hamel, Ernest
AU - Tabrizi, Mojgan Aghazadeh
AU - Balzarini, Jan
AU - Brancale, Andrea
AU - Preti, Delia
AU - Carrion, Maria Dora
AU - Baraldi, Pier Giovanni
AU - Romagnoli, Romeo
AU - Hsieh, Hsing-Pang
AU - Di Cristina, Antonietta
PY - 2008
Y1 - 2008
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10447/34018
M3 - Article
VL - Mar13;51(5)
SP - 1464
EP - 1468
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
ER -