Title: Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors
Authors: 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 #
Issue Date: Mar-2008
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:51 issue:5 pages:1464-1468
Abstract: 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.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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