2. Academic Validation
  3. Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors

Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors

  • J Med Chem. 2008 Mar 13;51(5):1464-8. doi: 10.1021/jm7011547.
Romeo Romagnoli 1,  Pier Giovanni Baraldi,  Taradas Sarkar,  Maria Dora Carrion,  Carlota Lopez Cara,  Olga Cruz-Lopez,  Delia Preti,  Mojgan Aghazadeh Tabrizi,  Manlio Tolomeo,  Stefania Grimaudo,  Antonella Di Cristina,  Nicola Zonta,  Jan Balzarini,  Andrea Brancale,  Hsing-Pang Hsieh,  Ernest Hamel
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Universita di Ferrarra, Italy. [email protected]
PMID: 18260616 DOI: 10.1021/jm7011547
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.

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